Sorafenib Tosylate(Synonyms: 甲苯磺酸索拉非尼; Bay 43-9006 Tosylate)

发表于2024年10月18日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Sorafenib Tosylate (Synonyms: 甲苯磺酸索拉非尼; Bay 43-9006 Tosylate) 纯度: 99.75%

Sorafenib Tosylate (Bay 43-9006 Tosylate) 是一种有效的口服活性 Raf 抑制剂，对 Raf-1 和 B-Raf 的 IC₅₀ 分别为 6 nM 和 20 nM。Sorafenib Tosylate 是一种多激酶抑制剂，对 VEGFR2，VEGFR3，PDGFRβ，FLT3 和 c-Kit 的 IC₅₀ 分别为 90 nM，15 nM，20 nM，57 nM 和 58 nM。Sorafenib Tosylate 诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)，并具有抗肿瘤活性。Sorafenib Tosylate 也是一种 ferroptosis 激动剂。

Sorafenib Tosylate Chemical Structure

CAS No. : 475207-59-1

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500 mg	￥1200	In-stock
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生物活性

Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC₅₀s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC₅₀s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator^[1].

IC₅₀ & Target^[1]

VEGFR3

20 nM (IC₅₀)

Braf

22 nM (IC₅₀)

Raf-1

6 nM (IC₅₀)

VEGFR2

90 nM (IC₅₀)

Braf^V599E

38 nM (IC₅₀)

PDGFRβ

57 nM (IC₅₀)

c-Kit

68 nM (IC₅₀)

Flt3

58 nM (IC₅₀)

体外研究
(In Vitro)

Sorafenib Tosylate also inhibits BRAF^wt (IC₅₀=22 nM), BRAF^V599E (IC₅₀=38 nM), VEGFR-2 (IC₅₀=90 nM), VEGFR-3 (IC₅₀=20 nM), PDGFR-β (IC₅₀=57 nM), c-KIT (IC₅₀=68 nM), and Flt3 (IC₅₀=58 nM) in biochemical assays^[1]. Sorafenib-induced phosphorylation of c-Met, p70S6K and 4EBP1 is significantly reduced when 10-0505 cells are co-treated with anti-human anti-HGF antibody, suggesting that treatment with Sorafenib Tosylate leads to increased HGF secretion and activation of c-Met and mTOR targets^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Sorafenib Tosylate (10, 30, 50 and 100 mg/kg, orally) treatment inhibits the tumor growth of 06-0606 and 10-0505 xenografts in a dose-dependent manner (P<0.01). The growth rate of 06-0606 and 10-0505 xenografts is also significantly reduced by Sorafenib. The weights of 06-0606 tumors in mice that are treated with Sorafenib 50 mg/kg and 100 mg/kg are approximately 13% and 5% of the controls, respectively. 50 mg dose of Sorafenib significantly inhibits tumor growth in mice with lines 5-1318, 26-1004 and 10-0505 (P<0.01). For 50 mg dose, the T/C ratio, where T and C are the median weight (mg) of Sorafenib- and vehicle-treated tumors at the end of the treatment, respectively, for 06-0606, 26-1004, 5-1318, and 10-0505 xenografts is 0.13, 0.10, 0.12 and 0.49, respectively^[2]. The survival rate is 73.3 % in Diethyl nitrosamine (DENA) group and 83.3 % in Sorafenib group compared to 100 % in the normal control group. DENA group shows a significant increase in liver index (1.51-fold increase, p<0.05) compared to normal control group, while treatment with Sorafenib shows significant decrease (p<0.05) in liver index when compared to DENA group. The liver index in Sorafenib group significantly decreases to lower than its value in the normal control^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

637.03

Formula

C₂₈H₂₄ClF₃N₄O₆S

CAS 号

475207-59-1

中文名称

甲苯磺酸索拉非尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 31 mg/mL (48.66 mM)

H₂O : < 0.1 mg/mL (insoluble)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5698 mL	7.8489 mL	15.6978 mL
5 mM	0.3140 mL	1.5698 mL	3.1396 mL
10 mM	0.1570 mL	0.7849 mL	1.5698 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: 2.08 mg/mL (3.27 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (3.27 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.27 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109.

[2]. Huynh H, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009 Aug;13(8B):2673-83.

[3]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16.

[4]. Zhu W, et al. Combination of sorafenib and Valproic acid synergistically induces cell apoptosis and inhibits hepatocellular carcinoma growth via down-regulating Notch3 and pAkt. Am J Cancer Res. 2017 Dec 1;7(12):2503-2514.

Kinase Assay ^[1]	To test compound inhibition against various RAF kinase isoforms, Sorafenib is added to a mixture of Raf-1 (80 ng), wt BRAF, or V599E BRAF (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl₂, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The RAF kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ-[³³P]ATP (400 Ci/mol) and incubated at 32°C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	The 10-0505, 06-0606, and 26-1004 tumors are finely minced and washed three times with modified Eagle medium (MEM). Cells are harvested by centrifuging at 800× g for 10 min. Cells are treated with 3 or 6 μM of Sorafenib in serum free MEM in the presence or absence of 5 μg/mL anti-human hepatocyte growth factor (HGF) antibody for 48 hrs. A total of 2 mL of conditioned medium from vehicle- or Sorafenib-treated (without anti-human antibody) is collected and concentrated using a VIVASPIN 20 and secreted HGF in conditioned medium is determined by western blotting^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]^[3]	Mice^[2] For dose-response experiment, mice bearing the 06-0606 and 10-0505 xenografts are given four doses of Sorafenib (10, 30, 50 and 100 mg/kg daily) orally for 12 days. Each treatment group comprised of five mice. To investigate the antitumor effects of Sorafenib, mice bearing tumors are orally administered 50 mg/kg Sorafenib daily for 12 days. Each treatment group is comprised of 14 animals and each experiment is repeated at least twice. Treatment started on day 7 after tumor implantation. By this time, the HCC xenografts reached the size of approximately 100 mm³. To study the effects of Rapamycin plus Sorafenib on the growth of 10-0505 xenograft, mice bearing tumors (14 per group) are orally administered either 200 μL of vehicle, or 50 mg/kg of Sorafenib, or 1 mg/kg of Rapamycin, or Rapamycin plus Sorafenib daily for indicated days. Tumor growth is monitored at least twice weekly by Vernier caliper measurement of the length and width of tumor. Tumor volume is calculated as follows: [length×width²×π/6]. At the end of the study, the mice are killed with body and tumor weights being recorded, and the tumors harvested for analysis. Rats^[3] In the study, 100- to 120-g male albino rats are utilized. After acclimatization period, rats are weighed and randomly divided into three groups: Group 1 (normal control group; n=10) is given the vehicle daily for 8 weeks. Group 2 (DENA group; n=15) receive i.p. single dose of 200 mg/kg DENA. Group 3 (Sorafenib group; n=12) is given Sorafenib orally at a dose of 10 mg/kg daily for 2 weeks, 6 weeks after DENA i.p. injection. At the end of the experiment (8 weeks), rats are weighed, anesthetized by ether, and killed, and their livers are dissected. Fresh liver is washed twice with ice-cold saline, dried on clean paper towel, and weighed. Liver index is calculated as liver weight (g)/final body weight (g)×100. The liver is divided into five portions: one portion is preserved in 10 % formalin for histopathological examination and the other portions are immediately frozen in liquid nitrogen and stored at −80°C. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wilhelm SM, et al. BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. [2]. Huynh H, et al. Sorafenib and rapamycin induce growth suppression in mouse models of hepatocellular carcinoma. J Cell Mol Med. 2009 Aug;13(8B):2673-83. [3]. El-Ashmawy NE, et al. Sorafenib effect on liver neoplastic changes in rats: more than a kinase inhibitor. Clin Exp Med. 2016 Apr 16. [4]. Zhu W, et al. Combination of sorafenib and Valproic acid synergistically induces cell apoptosis and inhibits hepatocellular carcinoma growth via down-regulating Notch3 and pAkt. Am J Cancer Res. 2017 Dec 1;7(12):2503-2514.

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Valemetostat tosylate(Synonyms: DS-3201 tosylate)

发表于2024年10月11日由上海金畔生物科技有限公司

Valemetostat tosylate (Synonyms: DS-3201 tosylate) 纯度: 99.91%

Valemetostat tosylate (DS-3201 tosylate) 是一种首创的 EZH1/2 抑制剂，用于复发/难治性周围 T 细胞淋巴瘤的研究。

Valemetostat tosylate Chemical Structure

CAS No. : 1809336-93-3

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Free Sample (0.1-0.5 mg)		Apply now
5 mg	￥2500	In-stock
10 mg	￥4200	In-stock
25 mg	￥8800	In-stock
50 mg	￥14500	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

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生物活性

Valemetostat tosylate (DS-3201 tosylate), a first-in-class EZH1/2 dual inhibitor, has the potential in the research of relapsed/refractory peripheral T-cell lymphoma^[1].

IC₅₀ & Target

EZH1/2^[1]

Clinical Trial

分子量

660.22

Formula

C₃₃H₄₂ClN₃O₇S

CAS 号

1809336-93-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 125 mg/mL (189.33 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5146 mL	7.5732 mL	15.1465 mL
5 mM	0.3029 mL	1.5146 mL	3.0293 mL
10 mM	0.1515 mL	0.7573 mL	1.5146 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.15 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.15 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.15 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW.

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S-Adenosyl-L-methionine tosylate(Synonyms: S-Adenosyl methionine tosylate; Ademetionine tosylate; AdoMet tosylate)

发表于2024年7月30日由上海金畔生物科技有限公司

S-Adenosyl-L-methionine tosylate (Synonyms: S-Adenosyl methionine tosylate; Ademetionine tosylate; AdoMet tosylate) 纯度: ≥98.0%

S-Adenosyl-L-methionine tosylate (S-Adenosyl methionine tosylate) 是通过蛋氨酸腺苷转移酶的作用由蛋氨酸和 ATP 内源性生产的，是一种重要的具有口服活性的甲基供体。S-Adenosyl-L-methionine tosylate 是一种具有有效的抗抑郁作用的膳食补充剂，可用于缓解疼痛的研究，并可用于肝病和骨关节炎的研究。

S-Adenosyl-L-methionine tosylate Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in Water	￥825	In-stock
50 mg	￥750	In-stock
100 mg	￥1300	In-stock
500 mg	￥3900	In-stock
1 g		询价
5 g		询价

* Please select Quantity before adding items.

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生物活性

S-Adenosyl-L-methionine tosylate (S-Adenosyl methionine tosylate) is produced endogenously from methionine and ATP by action of the enzyme methionine adenosyltransferase and is an important orally active methyl group donor. S-Adenosyl-L-methionine tosylate is a dietary supplement with potent antidepressant and analgesic effects, and has the potential for liver disease and osteoarthritis research^[1]^[2]^[3].

IC₅₀ & Target

Human Endogenous Metabolite

体外研究
(In Vitro)

S-Adenosyl-L-methionine (Ademetionine) is involved in three main metabolic pathways: 1) methylation, as the principal source of methyl groups in the body; 2) transsulfuration, S-Adenosyl-L-methionine forms S-Adenosylhomocysteine (SAH) and then converted to homocysteine (Hcy) which can be converted to cystathionine then to cysteine and the sulfate (SO4) donated to other metabolic intermediates; and 3) aminopropylation, as S-Adenosyl-L-methionine plays an important role in the synthesis of polyamines which can eventually form and recycle methionine^[2].
In vitro studies using human articular chondrocytes have shown S-Adenosyl-L-methionine-induced increases in proteoglycan synthesis and proliferation rates in rabbits^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Mice lacking methionine adenosyltransferase 1a (Mat1a) have reduced hepatic S-Adenosyl-L-methionine levels and develop oxidative stress, steatohepatitis, and hepatocellular carcinoma (HCC). However, injury and HCC also occur if hepatic S-Adenosyl-L-methionine level is excessive chronically. Thus a normal hepatic S-Adenosyl-L-methionine level is necessary to maintain liver health and prevent injury and HCC^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

570.64

Formula

C₂₂H₃₀N₆O₈S₂

中文名称

腺苷蛋氨酸甲苯磺酸盐；丁二磺酸腺苷蛋氨酸甲苯磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

H₂O : 250 mg/mL (438.10 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7524 mL	8.7621 mL	17.5242 mL
5 mM	0.3505 mL	1.7524 mL	3.5048 mL
10 mM	0.1752 mL	0.8762 mL	1.7524 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

参考文献

[1]. G M Bressa. et al. S-adenosyl-l-methionine (SAMe) as antidepressant: meta-analysis of clinical studies. Acta Neurol Scand Suppl. 1994;154:7-14.

[2]. Wadie I Najm, et al. S-adenosyl methionine (SAMe) versus celecoxib for the treatment of osteoarthritis symptoms: a double-blind cross-over trial. [ISRCTN36233495]. BMC Musculoskelet Disord. 2004 Feb 26;5:6.

[3]. Shelly C Lu, et al. S-adenosylmethionine in liver health, injury, and cancer. Physiol Rev. 2012 Oct;92(4):1515-42.

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T-1101 tosylate(Synonyms: TAI-95 tosylate)

发表于2024年7月28日由上海金畔生物科技有限公司

T-1101 tosylate (Synonyms: TAI-95 tosylate) 纯度: 99.61%

T-1101 tosylate (TAI-95 tosylate) 是一种具有抗肿瘤活性的 Hec1/Nek2 抑制剂。T-1101 tosylate 对正常细胞、激酶和 hERG 无抑制效果。

T-1101 tosylate Chemical Structure

CAS No. : 2250404-95-4

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥6590	In-stock
5 mg	￥4500	In-stock
10 mg	￥7500	In-stock
50 mg		询价
100 mg		询价

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生物活性

T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG^[1]

IC₅₀ & Target

Hec1/Nek2^[1]

体外研究
(In Vitro)

T-1101 tosylate shows potent in vitro antiproliferative activity (IC50: 14.8-21.5 nM)^[1].
T-1101 tosylate disrupts the Hec1/Nek2 protein–protein interaction in the cells^[1].
T-1101 tosylate (1μM; 3-24 24 hours) decreases the level of Nek2 in a time-dependent manner^[1].
T-1101 tosylate (1 µM; 24 hours) induces apoptosis^[1].
T-1101 tosylate reduces amounts of cell-cycle related proteins cyclin A1, cyclin B1, and cyclin D1^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis^[1]

Cell Line:	HeLa cells
Concentration:	1 µM
Incubation Time:	24 hours
Result:	Increased the amount of apoptotic marker proteins cleaved caspase-3 and PARP and decreased the amount of antiapoptotic proteins Mcl-1 and XIAP in HeLa cells.

Western Blot Analysis^[1]

Cell Line:	K562 cells
Concentration:	1 μM
Incubation Time:	3 hours, 6 hours, 16 hours, 24 hours
Result:	Lowered the level of Nek2 in a time-dependent manner.

体内研究
(In Vivo)

T-1101 tosylate shows good oral bioavailability and thermal stability ^[1].
Oral co-administration of T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) halves the dose of sorafenib (25 mg/kg to 12.5 mg/kg) required to exhibit comparable in vivo activity towards Huh-7 xenografts ^[1].
T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) shows significant in vivo activity in mice bearing various human cancer xenografts^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts^[1]
Dosage:	25 mg/kg, 50 mg/kg
Administration:	Oral administration; twice per day; 28 days
Result:	Showed significant in vivo activity in mice bearing various human cancer xenografts.

Clinical Trial

分子量

665.80

Formula

C₃₁H₃₁N₅O₆S₃

CAS 号

2250404-95-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (93.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5020 mL	7.5098 mL	15.0195 mL
5 mM	0.3004 mL	1.5020 mL	3.0039 mL
10 mM	0.1502 mL	0.7510 mL	1.5020 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.12 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.12 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Chuang SH, et al. Discovery of T-1101 tosylate as a first-in-class clinical candidate for Hec1/Nek2 inhibition in cancer therapy. Eur J Med Chem. 2020 Apr 1;191:112118.

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Niraparib tosylate(Synonyms: 尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate)

发表于2024年7月16日由上海金畔生物科技有限公司

Niraparib tosylate (Synonyms: 尼拉帕尼对苯甲磺酸盐; MK-4827 tosylate) 纯度: 99.81%

Niraparib tosylate (MK-4827 tosylate) 是一种高效的，具有生物口服利用度的 PARP1 和 PARP2 抑制剂，IC₅₀ 分别为 3.8 和 2.1 nM。Niraparib tosylate 抑制 DNA 损伤修复，诱导凋亡 (apoptosis) 并具有抗肿瘤活性。

Niraparib tosylate Chemical Structure

CAS No. : 1038915-73-9

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥672	In-stock
2 mg	￥550	In-stock
5 mg	￥620	In-stock
10 mg	￥1050	In-stock
50 mg	￥4100	In-stock
100 mg	￥5900	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Niraparib tosylate 相关产品

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Orally Active Compound Library
FDA Approved & Pharmacopeial Drug Library
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Rare Diseases Drug Library
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生物活性

Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC₅₀ of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity^[1]^[2]^[3].

IC₅₀ & Target

PARP-2

2.1 nM (IC₅₀)

PARP-1

3.8 nM (IC₅₀)

V-PARP

330 nM (IC₅₀)

TANK-1

570 nM (IC₅₀)

PARP-3

1300 nM (IC₅₀)

体外研究
(In Vitro)

Niraparib (MK-4827) inhibits PARP activity with EC₅₀=4 nM and EC₉₀=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC₅₀ in the 10−100 nM range. MK-4827 displays excellent PARP 1 and 2 inhibition with IC₅₀=3.8 and 2.1 nM, respectively, and in a whole cell assay^[1]. To validate that Niraparib (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM Niraparib (MK-4827) for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vd_ss=6.9 L/kg), long terminal half-life (t_1/2=3.4 h), and excellent bioavailability, F=65%^[1]. Niraparib (MK-4827) enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

492.59

Formula

C₂₆H₂₈N₄O₄S

CAS 号

1038915-73-9

中文名称

尼拉帕尼对苯甲磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 200 mg/mL (406.02 mM; Need ultrasonic)

H₂O : 1 mg/mL (2.03 mM; heat to 50°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0301 mL	10.1504 mL	20.3009 mL
5 mM	0.4060 mL	2.0301 mL	4.0602 mL
10 mM	0.2030 mL	1.0150 mL	2.0301 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution
3.

请依序添加每种溶剂： 1% DMSO 99% saline

Solubility: ≥ 0.5 mg/mL (1.02 mM); Clear solution

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.

[2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

[3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

[4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.

Cell Assay ^[2]	The inhibition of PARP is analyzed in A549 and H1299 cells using the HT Universal Chemiluminescent PARP Assay Kit. Briefly, cells are treated with DMSO or 1 μM Niraparib (MK-4827) for 15, 30, 60, or 120 minutes, trypsinized, and transferred to a pre-chilled tube. The cells are washed twice with ice cold PBS and resuspended in cold PARP extraction buffer. The cell suspensions are incubated on ice for 30 minutes with periodic vortexing to disrupt the cell membrane. The suspensions are centrifuged and the supernatant transferred to a pre-chilled tube on ice. The histone coated wells of the 96-well plate are rehydrated with 1X PARP buffer and incubated at room temperature for 30 minutes. The PARP buffer is removed and 20 μg of protein as determined by the Bio-Rad Protein Assay is added to each well followed by diluted PARP-HSA enzyme and 1X PARP buffer. The strip wells are then incubated at room temperature for 60 minutes, washed twice with PBS containing 0.1% Triton X-100, and then washed with PBS. Diluted Strep-HRP is added to the strip wells and incubated for 60 minutes at room temperature. The wells are washed again as before. Equal volumes of PeroxyGlow A and B are combined and added to the wells and chemiluminescent readings are obtained immediately using a plate-reader^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] Female nude mice (Ncr Nu/Nu) are randomly assigned to treatment groups consisting of 5 to 8 mice each when tumors grew to 6.0 mm in diameter at which time treatment with MK-4827 is initiated. MK-4827 is given at a dose of 25 mg/kg twice daily or 50 mg/kg once daily for either 21 days or is discontinued at 9 days from the time tumors reached 8 mm in diameter. Fractionated local tumor irradiation (XRT) is given when tumors reach 8.0 mm in diameter (7.7-8.2 mm). Radiation (2 Gy per fraction) is delivered to the tumor-bearing leg of mice once daily for 14 consecutive days or twice daily for 7 consecutive days using a small-animal irradiator consisting of two parallel-opposed 137Cs sources, at a dose rate of 5 Gy/min. During irradiation un-anesthetized mice are mechanically immobilized in a jig so that the tumor is centered within a 3.0 cm diameter radiation field and the animal’s body shielded from radiation exposure. On the day when both MK-4827 and radiation are given, drug is administered 1 h before the first radiation dose of the day. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85. [2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86. [3]. Wang L, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20. [4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164.

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LY-2584702 tosylate salt

发表于2024年7月9日由上海金畔生物科技有限公司

LY-2584702 tosylate salt 纯度: 98.12%

LY-2584702 tosylate salt 是一种 ATP 竞争性的选择性 p70S6K 抑制剂，IC₅₀ 为 4 nM。LY-2584702 抑制 S6K1 的 IC₅₀ 为 2 nM。

LY-2584702 tosylate salt Chemical Structure

CAS No. : 1082949-68-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1114	In-stock
5 mg	￥820	In-stock
10 mg	￥1200	In-stock
50 mg	￥3600	In-stock
100 mg	￥5600	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

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生物活性

LY-2584702 tosylate salt is a selective ATP competitive inhibitor of p70S6K with an IC₅₀ of 4 nM. In S6K1 enzyme assay, the IC₅₀ of LY-2584702 is 2 nM.

IC₅₀ & Target

S6K1

2 nM (IC₅₀)

p70S6K

4 nM (IC₅₀)

体外研究
(In Vitro)

LY-2584702 (LY2584702) inhibits phosphorylation of the S6 ribosomal protein (pS6) in HCT116 colon cancer cells with an IC₅₀ of 0.1-0.24 μM^[1]. In S6K1 enzyme assay, the IC₅₀ of LY-2584702 (LY2584702) is 2 nM. For pS6 inhibition in cells, the IC₅₀=100 nM. LY-2584702 has some activity against the S6K-related kinases MSK2 and RSK at high concentrations (enzyme assay IC₅₀=58-176 nM). LY-2584702 inhibits S6K activity in EOMA cells, as determined by the phosphorylation of its downstream effector S6, in a dose-dependent manner^[2]. Proliferation of A549 is significantly inhibited by LY-2584702 (LY2584702) treating over 24 h at 0.1 μM (P<0.05); and the trend of decline is more conspicuous with longer treatment and/or with the increased drug concentration (all P<0.05). Similar results are also observed in SK-MES-1, although the obvious inhibition is led by LY-2584702 at 0.6 μM (P<0.05), much higher than that of A549^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

LY-2584702 demonstrates significant single-agent efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models at two dose levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID. LY-2584702 demonstrates statistically significant tumour growth reduction at TMED50 (threshold minimum effective dose 50%) (2.3 mg/kg) and TMED90 (10 mg/kg) in the HCT116 colon carcinoma xenograft model^[1]. To examine the role of S6K in vivo, EOMA cells expressing shAkt3 are implanted in nu/nu mice, then treated for 14 days with LY-2584702 or Rapamycin. Analysis of tumors removed after 14 days shows that LY-2584702 inhibits S6 phosphorylation almost as effectively as Rapamycin. Loss of Akt3 increases tumor growth as compared with pLKO. LY-2584702 treatment alone does not significantly affect the growth of pLKO tumors. However, LY-2584702 significantly reduces the growth of tumors with shAkt3^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

617.62

Formula

C₂₈H₂₇F₄N₇O₃S

CAS 号

1082949-68-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 10.25 mg/mL (16.60 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6191 mL	8.0956 mL	16.1912 mL
5 mM	0.3238 mL	1.6191 mL	3.2382 mL
10 mM	0.1619 mL	0.8096 mL	1.6191 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1 mg/mL (1.62 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.62 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 1 mg/mL (1.62 mM); Suspended solution; Need ultrasonic

此方案可获得 1 mg/mL (1.62 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1 mg/mL (1.62 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75.

[2]. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50.

[3]. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.

Cell Assay ^[3]	LY-2584702 is fully dissolved in 20 mL 10% DMSO and reserved at -80°C. When conducted the experiments in vitro, LY-2584702 is further diluted in 0.5% Tween 80, 5% propylene glycol and 30% PEG400 to reach different DMSO concentrations of 0.1 μM, 0.2 μM, 0.6 μM, and 1.0 μM. Cell Counting Kit-8 (CCK-8) is used to measure the cells proliferation in vitro. Cell lines A549 and SK-MES-1 treated by LY-2584702 for 24 h with different concentrations are seeded in 96-well plates at a density of 5×10³ per well, with six repeats. DMSO treated, or in other words, the concentration of LY-2584702 of 0 is used as negative control. Cells absorbance at 450 nm is detected every 24 h after seeding to measure the proliferative activities^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] LY-2584702 is prepared in 0.25% Tween-80 and 0.05% antifoam, and administered orally to mice (12.5 mg/kg twice daily). EOMA cells (0.3×10⁶) are injected subcutaneously in 6- to 8-week-old nu/nu female mice (2 sites/mouse, 4-5 mice/group). Tumor size is measured daily. For drug treatment, when tumors reach 0.01 cm³ in size, the animals are treated with vehicle control or LY-2584702 (12.5 mg/kg twice daily, oral dosing). Tumor size is measured every 3 to 4 days^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75. [2]. Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50. [3]. Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.

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甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

发表于2024年6月10日由上海金畔生物科技有限公司

甲苯磺酰基 PEG, mPEG-Tosylate

MW 1000 Da

有货

品牌：Jinpan

Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU)	包装规格	是否现货
T164401-100mg	100mg	期货
T164401-500mg	500mg	期货
T164401-2.5g	2.5g	期货

基本信息

产品名称	甲苯磺酰基 PEG, mPEG-Tosylate
英文名称	Tosyl PEG, mPEG-Tosylate
规格或纯度	MW 1000 Da
运输条件	常规运输

一般描述

Tosyl functionctional PEG is an amino (-NH₂) group reactive PEG derivative that can be used to modify protein, peptide or any other surfaces with available amino groups. Tosyl PEGs react readily with amine groups at a pH of from 8.0 to 9.5.

溶解性	Off-white/white solid or viscous liquid depends on molecule weight;Soluble in regular aqeous solution as well as most organic solvents;
品牌	Jinpan

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

发表于2024年6月7日由上海金畔生物科技有限公司

甲苯磺酰基 PEG, mPEG-Tosylate

MW 5000 Da

有货

品牌：Jinpan

Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU)	包装规格	是否现货	价格	数量
T164405-1g	1g	期货
T164405-5g	5g	期货

基本信息

产品名称	甲苯磺酰基 PEG, mPEG-Tosylate
英文名称	Tosyl PEG, mPEG-Tosylate
规格或纯度	MW 5000 Da
运输条件	常规运输

一般描述

溶解性	Off-white/white solid or viscous liquid depends on molecule weight;Soluble in regular aqeous solution as well as most organic solvents;
品牌	Jinpan

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

发表于2024年6月1日由上海金畔生物科技有限公司

甲苯磺酰基 PEG, mPEG-Tosylate

MW 10000 Da

有货

品牌：Jinpan

Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU)	包装规格	是否现货	价格	数量
T164402-1g	1g	期货

基本信息

产品名称	甲苯磺酰基 PEG, mPEG-Tosylate
英文名称	Tosyl PEG, mPEG-Tosylate
规格或纯度	MW 10000 Da
运输条件	常规运输

一般描述

溶解性	Off-white/white solid or viscous liquid depends on molecule weight;Soluble in regular aqeous solution as well as most organic solvents;
品牌	Jinpan

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

发表于2024年6月1日由上海金畔生物科技有限公司

甲苯磺酰基 PEG, mPEG-Tosylate

MW 2000 Da

有货

品牌：Jinpan

Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU)	包装规格	是否现货	价格	数量
T164403-1g	1g	期货

基本信息

产品名称	甲苯磺酰基 PEG, mPEG-Tosylate
英文名称	Tosyl PEG, mPEG-Tosylate
规格或纯度	MW 2000 Da
运输条件	常规运输

一般描述

甲苯磺酰基 PEG, mPEG-Tosylate, ,Tosyl PEG, mPEG-Tosylate,

发表于2024年6月1日由上海金畔生物科技有限公司

甲苯磺酰基 PEG, mPEG-Tosylate

MW 20000 Da

有货

品牌：Jinpan

Tosyl PEG, mPEG-Tosylate

MSDS

质检证书(CoA)

相似产品

货号 (SKU)	包装规格	是否现货	价格	数量
T164404-1g	1g	期货

基本信息

产品名称	甲苯磺酰基 PEG, mPEG-Tosylate
英文名称	Tosyl PEG, mPEG-Tosylate
规格或纯度	MW 20000 Da
运输条件	常规运输

一般描述

TMPyP4 tosylate(Synonyms: TMP 1363)

发表于2024年5月16日由上海金畔生物科技有限公司

TMPyP4 tosylate (Synonyms: TMP 1363) 纯度: ≥98.0%

TMPyP4 tosylate (TMP 1363) 是一种四链体 (G-quadruplex) 特异性配体，可抑制 G-四链体和 IGF-1 之间的相互作用。TMPyP4 tosylate (TMP 1363) 是一种端粒酶 (telomerase) 抑制剂，在骨肉瘤细胞系中具有抗肿瘤作用。

TMPyP4 tosylate Chemical Structure

CAS No. : 36951-72-1

规格	价格	是否有货
100 mg	￥1200	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

TMPyP4 tosylate 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Cell Cycle/DNA Damage Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library

生物活性

TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1^[1]. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines^[2].

IC₅₀ & Target

G-quadruplex^[2]
Telomerase^[2]

分子量

1363.60

Formula

C₇₂H₆₆N₈O₁₂S₄

CAS 号

36951-72-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 25 mg/mL (18.33 mM; Need ultrasonic)

DMSO : 10 mg/mL (7.33 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.7334 mL	3.6668 mL	7.3335 mL
5 mM	0.1467 mL	0.7334 mL	1.4667 mL
10 mM	0.0733 mL	0.3667 mL	0.7334 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1 mg/mL (0.73 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (0.73 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (0.73 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (0.73 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Chen H, et al. Insuline-like growth factor type I selectively binds to G-quadruplex structures. Biochim Biophys Acta Gen Subj. 2019 Jan;1863(1):31-38.

[2]. Fujimori J, et al. Antitumor effects of telomerase inhibitor TMPyP4 in osteosarcoma cell lines. J Orthop Res. 2011 Nov;29(11):1707-11.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

HO-PEG4-Tosylate Cat. No. PG4-OHTS-1 100 mg修饰性聚乙二醇

发表于2024年5月15日由上海金畔生物科技有限公司

上海金畔生物科技有限公司提供各种分子量和基团修饰性聚乙二醇定制服务。

HO-PEG4-Tosylate

Cat. No.	PG4-OHTS-1
Specification
Unit Size	100 mg
Price	$385.00

Documents

SDS
DataSheet

Milademetan tosylate hydrate(Synonyms: DS-3032b; DS-3032 tosylate hydrate)

发表于2024年5月4日由上海金畔生物科技有限公司

Milademetan tosylate hydrate (Synonyms: DS-3032b; DS-3032 tosylate hydrate) 纯度: 98.21%

Milademetan (DS-3032) tosylate hydrate 是特异性的、具有口服活性的 MDM2 抑制剂，用于急性髓系白血病和实体肿瘤的研究。Milademetan (DS-3032) tosylate hydrate 可诱导 G1 细胞周期阻滞、衰老和凋亡。

Milademetan tosylate hydrate Chemical Structure

CAS No. : 2095625-97-9

规格	价格	是否有货
5 mg	￥5800	In-stock
10 mg	￥9800	In-stock
25 mg	￥20000	In-stock
50 mg	￥33500	In-stock
100 mg	￥56000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Milademetan tosylate hydrate 相关产品

•相关化合物库:

Covalent Screening Library Plus
Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Apoptosis Compound Library
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Autophagy Compound Library
Anti-Aging Compound Library
Drug Repurposing Compound Library
Covalent Screening Library
Oxygen Sensing Compound Library
Ubiquitination Compound Library
Ferroptosis Compound Library
Pyroptosis Compound Library
Glutamine Metabolism Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library
Anti-Liver Cancer Compound Library
Rare Diseases Drug Library
Anti-Colorectal Cancer Compound Library

生物活性

Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis^[1]^[2].

体外研究
(In Vitro)

Milademetan (DS-3032) can stabilize TP53 and selectively induce CDKNA1, BAX and MDM2 expression in neuroblastoma cells with wild-type TP53^[3].
Milademetan (DS-3032b) treatment enhances TP53 target gene expression and induces G1 cell cycle arrest, senescence and apoptosis^[3].
Milademetan (DS-3032b, 0-2000 nM) treatment selectively inhibits viability, proliferation and migration of neuroblastoma cells with wildtype TP53 independently of MYCN status^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[4]

Cell Line:	SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines.
Concentration:	0-2000 nM.
Incubation Time:	24-72 h.
Result:	Reduced viability in a dose- and time-dependent manner. Exhibited IC50 values of 21.9 nM, 17.7 nM, 52.63 nM, 25.7 nM and 44.1 nM in SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines, respectively (72 h).

体内研究
(In Vivo)

Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SH-SY5Y xenograft tumors in nude mice^[4].
Dosage:	50 mg/kg.
Administration:	Oral gavage for 30 consecutive days with an alternating schedule of 4 days of daily treatment with oral gavages followed by 2 days without treatment (4+2).
Result:	Survival in the mouse cohort was significantly prolonged. Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling.

Clinical Trial

分子量

808.74

Formula

C₃₇H₄₄Cl₂FN₅O₈S

CAS 号

2095625-97-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 50 mg/mL (61.82 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2365 mL	6.1825 mL	12.3649 mL
5 mM	0.2473 mL	1.2365 mL	2.4730 mL
10 mM	0.1236 mL	0.6182 mL	1.2365 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: 5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (6.18 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (6.18 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 5 mg/mL (6.18 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (6.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. ARYL SULFONOHYDRAZIDES. WO 2017069289 A1.

[2]. M.M. Gounder, et al. Milademetan, an oral MDM2 inhibitor, in well-differentiated/dedifferentiated liposarcoma: results from a phase 1 study in patients with solid tumors or lymphomas. European Journal of Cancer 138S2 (2020) S1–S62.

[3]. Li, Yangbing, et al. Development of novel PROTAC Small-Molecule Degraders of MDM2 Protein and Peptidomimetic Inhibitors Targeting WDR5-MLL1 Protein-Protein Interaction.

[4]. Viktor Arnhold, et al. Reactivating TP53 signaling by the novel MDM2 inhibitor DS-3032b as a therapeutic option for high-risk neuroblastoma. ncotarget. 2018 Jan 5; 9(2): 2304–2319.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Dactolisib Tosylate(Synonyms: BEZ235 Tosylate; NVP-BEZ 235 Tosylate)

发表于2024年4月14日由上海金畔生物科技有限公司

Dactolisib Tosylate (Synonyms: BEZ235 Tosylate; NVP-BEZ 235 Tosylate) 纯度: 99.88%

Dactolisib Tosylate (BEZ235 Tosylate) 是PI3K和mTOR的双重激酶抑制剂，对PI3Kα, β, γ, δ 的IC₅₀值分别为4, 75, 7, 5 nM。Dactolisib Tosylate (BEZ235 Tosylate) 抑制 mTORC1 和 mTORC2。

Dactolisib Tosylate Chemical Structure

CAS No. : 1028385-32-1

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥500	In-stock
10 mg	￥450	In-stock
50 mg	￥950	In-stock
100 mg	￥1450	In-stock
200 mg	￥2100	In-stock
500 mg	￥3900	In-stock
1 g		询价
5 g		询价

* Please select Quantity before adding items.

Dactolisib Tosylate 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Kinase Inhibitor Library
PI3K/Akt/mTOR Compound Library
Stem Cell Signaling Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Autophagy Compound Library
Anti-Aging Compound Library
Drug Repurposing Compound Library
Antioxidants Compound Library
Differentiation Inducing Compound Library
Reprogramming Compound Library
Oxygen Sensing Compound Library
Glycolysis Compound Library
Cytoskeleton Compound Library
Glutamine Metabolism Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Anti-Cancer Metabolism Compound Library
Angiogenesis Related Compound Library
Lipid Metabolism Compound Library
Glucose Metabolism Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC₅₀ values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.

IC₅₀ & Target

p110α

4 nM (IC₅₀)

p110β

75 nM (IC₅₀)

p110δ

7 nM (IC₅₀)

p110γ

5 nM (IC₅₀)

p110α-H1047R

4.6 nM (IC₅₀)

p110α-E545K

5.7 nM (IC₅₀)

mTOR

20.7 nM (IC₅₀)

mTORC1

mTORC2

Autophagy

体外研究
(In Vitro)

Dactolisib (BEZ235) is an imidazo[4,5-c]quinoline derivative that inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes. The IC₅₀s for PI3Kα, β, γ, δ are 4, 75, 7, 5 nM, respectively. It is also found to be as active against the mutant PI3Kα^E545K or PI3Kα^H1047R with IC₅₀s of 5.7 and 4.6 nM, respectively. In human tumor cell lines, it is able to effectively and specifically block the dysfunctional activation of the PI3K pathway, inducing G1 arrest. PTEN-null cell lines PC3M and U87MG shows a dose-dependent reduction in cell proliferation when treated with increasing concentrations of Dactolisib (BEZ235), with an average GI₅₀ of 10 to 12 nM^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Dactolisib (BEZ235) is well tolerated, displays disease stasis when administered orally, and enhances the efficacy of other anticancer agents. At a dose of 50 mg/kg, Dactolisib (BEZ235) appears rapidly in plasma with a C_max of 1.68 μM at 0.5 h and a C_24h of 0.03 μM^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

641.74

Formula

C₃₇H₃₁N₅O₄S

CAS 号

1028385-32-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 34 mg/mL (52.98 mM; Need ultrasonic and warming)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5583 mL	7.7913 mL	15.5826 mL
5 mM	0.3117 mL	1.5583 mL	3.1165 mL
10 mM	0.1558 mL	0.7791 mL	1.5583 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 50% PEG300 50% saline

Solubility: 16.67 mg/mL (25.98 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 1 mg/mL (1.56 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7(7), 1851-1863.

Animal Administration
^[1]

Mice: The NVP-Dactolisib (BEZ235) powder is dissolved in NMP on sonication, and the remaining volume of polyethylene glycol 300 is added to a concentration of 5 mg/mL. The application volume is 10 mL/kg. For analytics, frozen tissues are minced and then homogenized in an equal volume of ice-cold PBS and centrifugation, supernatants are analyzed. Samples are then eluted with a linear gradient of 10% to 90% (v/v) acetonitrile in water containing 0.05% (v/v) trifluoroacetic acid over a period of 20 min at a flow rate of 1 mL/min. The compounds are detected by UV absorbance at 340 nm, and concentrations are determined by the external standard method using peak heights^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Maira SM, et al. Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity. Mol Cancer Ther, 2008, 7(7), 1851-1863.

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Allitinib tosylate(Synonyms: 艾力替尼; AST-1306 (TsOH))

发表于2024年4月10日由上海金畔生物科技有限公司

Allitinib tosylate (Synonyms: 艾力替尼; AST-1306 (TsOH)) 纯度: 99.83%

Allitinib tosylate (AST-1306 (TsOH)) 是一种具有口服活性且不可逆的 EGFR 和 ErbB2 抑制剂IC₅₀ 分别为 0.5 和 3 nM。Allitinib tosylate 抑制 ErbB4，IC₅₀ 为 0.8 nM。Allitinib tosylate 是一种苯胺基喹唑啉化合物，具有抗癌活性。

Allitinib tosylate Chemical Structure

CAS No. : 1050500-29-2

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥2643	In-stock
2 mg	￥1280	In-stock
5 mg	￥1934	In-stock
10 mg	￥2911	In-stock
50 mg	￥8510	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

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生物活性

Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC₅₀s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC₅₀ of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity^[1]

IC₅₀ & Target

EGFR

0.5 nM (IC₅₀)

ErbB2

3 nM (IC₅₀)

EGFR^L858R/T790M

12 nM (IC₅₀)

ErbB4

0.8 nM (IC₅₀)

体外研究
(In Vitro)

AST1306 tosylate (AST-1306 (TsOH); 0.19-6.25 μM; 72 hours) induces a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells^[1].
AST1306 tosylate inhibits the activation of tyrosine kinases and downstream signaling pathways in A549 cells, Calu-3 cells and SK-OV-3 cells. AST1306 tosylate dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells^[1].
AST1306 tosylate (0.1, 0.5, 1.0, 5.0 μM) can dramatically inhibit the growth of both tumor cells on soft agar, and SK-OV-3 cells exhibited much more sensitivity than that of A549 cells^[1].
AST1306 tosylate (0.001-1.0 μM; 4 hours) is more than 3000-fold selective for ErbB family kinases over other kinase families^[1].
AST1306 tosylate potently inhibits the EGFR T790M/L858R double mutant, exhibiting an IC₅₀ value of 12±2 nmol/L^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	NIH3T3 parental cells and NIH3T3 cells
Concentration:	0.19, 0.39, 0.78, 1.56, 3.13, 6.25 μM
Incubation Time:	72 hours
Result:	Induced a significant, concentration-dependent inhibition of the growth of HIH3T3-EGFR T790M/L858R cells.

Western Blot Analysis^[1]

Cell Line:	A549 cells , Calu-3 cells and SK-OV-3 cells
Concentration:	0.001, 0.01, 0.1, 1.0 μM
Incubation Time:	4 hours
Result:	Inhibits the activation of tyrosine kinases and downstream signaling pathways.

体内研究
(In Vivo)

AST1306 tosylate (AST-1306 (TsOH); p.o.; 25-100 mg/kg; twice daily; for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice with SK-OV-3 and Calu-3 tumors^[1]
Dosage:	25, 50, 100 mg/kg
Administration:	p.o.; twice daily; for 28 days
Result:	Caused a dramatic suppression of tumor growth.

Clinical Trial

分子量

621.08

Formula

C₃₁H₂₆ClFN₄O₅S

CAS 号

1050500-29-2

中文名称

艾力替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 50 mg/mL (80.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6101 mL	8.0505 mL	16.1010 mL
5 mM	0.3220 mL	1.6101 mL	3.2202 mL
10 mM	0.1610 mL	0.8050 mL	1.6101 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Xie H, Lin L, Tong L et al. AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. PLoS One. 2011;6(7):e21487.

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生物活性分子抑制剂Talazoparib tosylate(Synonyms: BMN 673ts)

发表于2024年4月10日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
Talazoparib tosylate (Synonyms: BMN 673ts) 纯度: 99.72%

Talazoparib tosylate (BMN 673ts) 是一种新型，高效，有可口服活性的 PARP1/2 抑制剂，抑制PARP1的IC₅₀ 值为 0.57 nM。

Talazoparib tosylate Chemical Structure

CAS No. : 1373431-65-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1884	In-stock
2 mg	￥1030	In-stock
5 mg	￥1550	In-stock
10 mg	￥2450	In-stock
50 mg	￥6500	In-stock
100 mg	￥11000	In-stock
200 mg	￥17000	In-stock
500 mg		询价
1 g		询价

* Please select Quantity before adding items.

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Targeted Therapy Drug Library

生物活性

Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC₅₀ of 0.57 nM for PARP1.

IC₅₀ & Target

IC50: 0.57 nM (PARP1)^[1]

体外研究
(In Vitro)

Talazoparib is a potent PARP1/2 inhibitor (PARP1 IC₅₀=0.57 nM), it has no effect on PARG activity at concentrations up to 1 μM. Talazoparib binds to PARP1 with a dissociation constant (K_D) of 0.29 nM. Talazoparib inhibits PARP1 and -2 to a similar extent, with K_is of 1.20 and 0.85 nM, respectively. Talazoparib selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors. Talazoparib targets tumor cells with homologous recombination gene defects. Tumor models that are either BRCA1-deficient (MX-1 and SUM149) or BRCA2-deficient (Capan-1) are profoundly sensitive to Talazoparib. Talazoparib induces nuclear γ-H2AX foci at concentrations as low as 100 pM^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Talazoparib is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice. Synergistic or additive antitumor effects are also found when Talazoparib is combined with temozolomide, SN38, or platinum drugs^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

552.55

Formula

C₂₆H₂₂F₂N₆O₄S

CAS 号

1373431-65-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 108 mg/mL (195.46 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8098 mL	9.0490 mL	18.0979 mL
5 mM	0.3620 mL	1.8098 mL	3.6196 mL
10 mM	0.1810 mL	0.9049 mL	1.8098 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Shen Y, et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res. 2013 Sep 15;19(18):5003-15.

Cell Assay ^[1]	LoVo cells are treated with Talazoparib (10, 40 nM) and temozolomide (TMZ) either alone or in combination for 5 days. Surviving fraction is determined using CellTiter-Glo assay.^[1] 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] In single-agent studies, olaparib (100 mg/kg), Talazoparib (0.33 or 0.1 mg/kg/d), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) is administered by oral gavage (per os), once daily or Talazoparib (0.165 mg/kg) twice daily for 28 consecutive days. Mice are continuously monitored for 10 more days after last day of dosing^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Shen Y, et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res. 2013 Sep 15;19(18):5003-15.

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Clofilium tosylate(Synonyms: 氯非铵甲苯磺酸盐)

发表于2024年4月7日由上海金畔生物科技有限公司

Clofilium tosylate (Synonyms: 氯非铵甲苯磺酸盐) 纯度: ≥98.0%

Clofilium tosylate 是一种钾通道 (potassium channel) 阻滞剂，作用于人早幼粒细胞白血病 (HL-60) 细胞，激活 caspase-3 而诱导凋亡。具有抗心律失常作用。

Clofilium tosylate Chemical Structure

CAS No. : 92953-10-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1210	In-stock
10 mg	￥1100	In-stock
50 mg	￥4900	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

Clofilium tosylate 相关产品

•相关化合物库:

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Neurodegenerative Disease-related Compound Library

生物活性

Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent^[1].

IC₅₀ & Target

Potassium channel^[1]

体外研究
(In Vitro)

HL-60 cells treated with Clofilium (0-20 μM; 24, 48, and 72 hours) lead to suppression of viability and proliferation in both time and concentration-dependent manners. Cell viability decreases significantly in HL-60 cells treated with 2.5 μM to 10 μM of Clofilium^[1].
Clofilium (10 μM, 12 hours) induces the proteolytic cleavage of inactive procaspase-3, p34 into its active form, p17 and subsequent cleavage of its substrate PARP at 2 h after exposure to 10 mM Clofilium. However, there is no significant change in expression of Bcl-2 and Bax proteins^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	HL-60 cells
Concentration:	0-20 μM
Incubation Time:	24, 48, and 72 hours
Result:	Inhibited HL-60 cells with IC₅₀s of 6.3 μM for 24 hours, 3.4 μM for 48 hours, 2.4 μM for 72 hours, respectively.

Western Blot Analysis^[1]

Cell Line:	HL-60 cells
Concentration:	10 μM
Incubation Time:	12 hours
Result:	Induced proteolytic cleavage of caspase-3 and subsequent cleavage of its substrate, PARP, while Bcl-2 and Bax proteins were unaltered.

分子量

510.17

Formula

C₂₈H₄₄ClNO₃S

CAS 号

92953-10-1

中文名称

氯非铵甲苯磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 125 mg/mL (245.02 mM; Need ultrasonic)

H₂O : 1.59 mg/mL (3.12 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9601 mL	9.8007 mL	19.6013 mL
5 mM	0.3920 mL	1.9601 mL	3.9203 mL
10 mM	0.1960 mL	0.9801 mL	1.9601 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.08 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.08 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

请依序添加每种溶剂： 8g/L NaCl solution

Solubility: 2 mg/mL (3.92 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Choi BY, et al. Clofilium, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Cancer Lett. 1999 Dec 1;147(1-2):85-93.

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Domatinostat tosylate(Synonyms: 4SC-202)

发表于2024年3月14日由上海金畔生物科技有限公司

Domatinostat tosylate (Synonyms: 4SC-202) 纯度: 99.66%

Domatinostat tosylate (4SC-202) 是一种 I 型 HDAC 抑制剂，能够抑制 HDAC1，HDAC2，和 HDAC3 的活性，IC₅₀ 值分别为 1.20 μM，1.12 μM 和 0.57 μM；同时能够抑制组蛋白赖氨酸特异性脱甲基酶1 (Lysine specific demethylase 1) 的活性。

Domatinostat tosylate Chemical Structure

CAS No. : 1186222-89-8

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1636	In-stock
2 mg	￥800	In-stock
5 mg	￥1200	In-stock
10 mg	￥1800	In-stock
50 mg	￥5100	In-stock
100 mg	￥8150	询价
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Domatinostat tosylate 相关产品

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Reprogramming Compound Library
Oxygen Sensing Compound Library
Anti-Breast Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Anti-Liver Cancer Compound Library

生物活性

Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC₅₀ of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).

IC₅₀ & Target^[4]

HDAC-3

0.57 μM (IC₅₀)

HDAC-2

1.12 μM (IC₅₀)

HDAC-1

1.2 μM (IC₅₀)

HDAC-11

9.7 μM (IC₅₀)

HDAC-5

11.3 μM (IC₅₀)

HDAC-10

21 μM (IC₅₀)

HDAC-9

50 μM (IC₅₀)

体外研究
(In Vitro)

Domatinostat tosylate significantly reduces proliferation of all epithelial and mesenchymal UC cell lines (IC₅₀ 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity^[1]. Domatinostat tosylate provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat tosylate-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat tosylate induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat tosylate. Domatinostat tosylate-induced cytotoxicity is dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreases the sensitivity by Domatinostat tosylate in HT-29 cells. Notably, Domatinostat tosylate, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity^[2]. Domatinostat tosylate treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat tosylate induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Oral gavage of Domatinostat tosylate inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

619.71

Formula

C₃₀H₂₉N₅O₆S₂

CAS 号

1186222-89-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 51 mg/mL (82.30 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6137 mL	8.0683 mL	16.1366 mL
5 mM	0.3227 mL	1.6137 mL	3.2273 mL
10 mM	0.1614 mL	0.8068 mL	1.6137 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Pinkerneil M, et al. Evaluation of the Therapeutic Potential of the Novel Isotype Specific HDAC Inhibitor 4SC-202 in Urothelial Carcinoma Cell Lines. Target Oncol. 2016 Dec;11(6):783-798.

[2]. S.W.Henning, et al. Preclinical characterization of 4SC-202, a noval isotype specific HDAC inhibitor.

[3]. Zhijun H, et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 2016 Aug;37(8):10257-67.

[4]. Fu M, et al. 4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to inhibit hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2016 Mar 4;471(2):267-73

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Ningetinib Tosylate(Synonyms: 对甲苯磺酸宁格替尼)

发表于2024年3月10日由上海金畔生物科技有限公司

Ningetinib Tosylate (Synonyms: 对甲苯磺酸宁格替尼) 纯度: 99.92%

Ningetinib Tosylate 是一种有效的口服生物可用的小分子酪氨酸激酶抑制剂 (TKI)，对 c-Met，VEGFR-2 和 Axl 的 IC₅₀ 值分别为 6.7, 1.9 和 <1.0 nM。

Ningetinib Tosylate Chemical Structure

CAS No. : 1394820-77-9

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1363	In-stock
5 mg	￥850	In-stock
10 mg	￥1200	In-stock
50 mg	￥4200	In-stock
100 mg	￥7200	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Ningetinib Tosylate 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
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Kinase Inhibitor Library
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Differentiation Inducing Compound Library
Reprogramming Compound Library
Orally Active Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC₅₀s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

IC₅₀ & Target

VEGFR2

1.9 nM (IC₅₀)

体外研究
(In Vitro)

Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC₅₀s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. In cell-based functional assays, Ningetinib Tosylate (CT053PTSA) inhibits HGF and VEGF-stimulated HUVEC proliferation and microvascular angiogenesis in rat aortic rings with IC₅₀ values of 8.6 and 6.3 nM, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

When single dosed orally (3 mg/kg) to U87MG tumor-bearing nude mice, Ningetinib Tosylate (CT053PTSA) potently inhibits the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours in tumor tissues. In orthotopic U87MG human glioblastoma xenograft model, Ningetinib Tosylate prolongs the median survival time (MST) and yields significant increase in life-span value (ILS=32%, p=0.003) at an oral dose of 20 mg/kg/day (dosed 21 days) versus the vehicle-treated group^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

728.79

Formula

C₃₈H₃₇FN₄O₈S

CAS 号

1394820-77-9

中文名称

对甲苯磺酸宁格替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (45.73 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3721 mL	6.8607 mL	13.7214 mL
5 mM	0.2744 mL	1.3721 mL	2.7443 mL
10 mM	0.1372 mL	0.6861 mL	1.3721 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (3.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.43 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (3.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.43 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (3.43 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.43 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Ning Xi, et al. Abstract 1755: CT053PTSA, a novel c-MET and VEGFR2 inhibitor, potently suppresses angiogenesis and tumor growth. Cancer Res 2014;74(19 Suppl):Abstract nr 1755.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

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