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Agerafenib hydrochloride(Synonyms: CEP-32496 hydrochloride; RXDX-105 hydrochloride)

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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。

Agerafenib hydrochloride (Synonyms: CEP-32496 hydrochloride; RXDX-105 hydrochloride)

Agerafenib (CEP-32496) hydrochloride 是一种口服高效的 BRAFV600E 抑制剂，Kd 为 14 nM。

Agerafenib hydrochloride(Synonyms: CEP-32496 hydrochloride; RXDX-105 hydrochloride)

Agerafenib hydrochloride Chemical Structure

CAS No. : 1227678-26-3

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Agerafenib hydrochloride 的其他形式现货产品:

Agerafenib

生物活性

Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.

IC50 & Target

BRafV600E

14 nM (Kd)

Braf

36 nM (Kd)

CRAF

39 nM (Kd)

c-Kit

2 nM (Kd)

Ret

2 nM (Kd)

LCK

2 nM (Kd)

Abl-1

3 nM (Kd)

VEGFR-2

8 nM (Kd)

CSF-1R

9 nM (Kd)

EPHA2

14 nM (Kd)

EGFR

22 nM (Kd)

c-Met

513 nM (Kd)

JAK-2

4700 nM (Kd)

MEK-1

7100 nM (Kd)

MEK-2

8300 nM (Kd)

体外研究
(In Vitro)

Agerafenib (CEP-32496) exhibits high potency against several BRAFV600E-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAFV600E versus those containing wild-type BRAF. Agerafenib (CEP-32496) exhibits potent binding (BRAFV600E Kd=14 nM) and cellular activity (pMEK IC50=82 nM and A375 proliferation IC50=78 nM), with activity in the proliferation assay. CEP-32496 also exhibits a favorable CYP450 inhibition profile, with measured IC50 values greater than 10 μM versus the CYP1A2, CYP2C9, CYP2D6, and CYP3A4 isoforms and an IC50=3.4 μM versus CYP2C19[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)

Oral administration of Agerafenib (CEP-32496) to Colo-205 tumor xenograft-bearing mice results in significant inhibition of pMEK in tumor cell lysates. For instance, a single 30 mg/kg (po) dose of Agerafenib (CEP-32496) leads to a 50 and 75% inhibition of normalized pMEK in tumor lysates at the 2 and 6 h postdose time point, respectively (p<0.03), while a 55 mg/kg (po) dose resulted in a 75% to 57% (p<0.03) inhibition of pMEK at 2 through 10 h post administration, with normalization to baseline by 24 h. Agerafenib (CEP-32496) exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib (CEP-32496) to beagle dogs (single dose of 1 mg/kg iv and 10 mg/kg po) results in low clearance (CL=5.0 (mL/min)/kg) and excellent bioavailability (%F=100). Similarly, in cynomolgus monkey, the administration of Agerafenib (CEP-32496) (single dose of 1 mg/kg iv and 10 mg/kg po) leads to high oral exposure due to low clearance (CL=6.7 mL/min/kg) and excellent bioavailability (%F=100)[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

553.92

Formula

C24H23ClF3N5O5
CAS 号

1227678-26-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Rowbottom MW, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Cell Assay
[1]

A375 cells are seeded at 10,000 cells per well in DMEM with 10% fetal calf serum and allowed to attach. The cells are washed with PBS and switched to DMEM with 0.5% of serum and incubated overnight. The test compounds (e.g., Agerafenib (CEP-32496); 10 μM) are then added at various concentrations with a final DMSO concentration of 0.5% and incubated for 72 h. At the end of incubation, a Cell Titer Blue is added per instructions, and incubation is continued for 3 h. Remaining viable cells are quantified by measuring the strength of the fluorescence signal using SoftMax Pro (excitation at 560 nm and emission at 590 nm). IC50 values are derived using a 9-point curve and are presented as mean values from experiments performed in duplicate[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]
Six to eight week old athymic nu/nu nude mice (20-25 g) are inoculated subcutaneously with Colo-205 tumor cells (1×106/mouse) in the right flank. Upon reaching an average tumor volume of 150-200 mm3 (10-12 days post implantation), animals are randomized into treatment groups (n=10 mice/group). Each group is dosed orally for 14 days with either vehicle only (22% HPβCD) or with Agerafenib (CEP-32496) at 10, 30, or 100 mg/kg twice daily (BID), and each dose of drug is given in a volume of 0.1 mL per 20 g of body weight, adjusted for the body weight of the animal. Tumor volumes are measured three times weekly using vernier calipers, and volumes are calculated[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]. Rowbottom MW, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

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Delanzomib(Synonyms: CEP-18770)

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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。

Delanzomib (Synonyms: CEP-18770) 纯度: ≥98.0%

Delanzomib (CEP-18770) 是一种强效的具有口服活性的蛋白酶体的胰凝乳蛋白酶样活性 (chymotrypsin-like activity of the proteasome) 抑制剂，IC50 为 3.8 nM。Delanzomib 抑制 NF-κB 活性，诱导癌细胞凋亡 (apoptotic)，并具有很强的抗血管生成和抗癌活性。

Delanzomib(Synonyms: CEP-18770)

Delanzomib Chemical Structure

CAS No. : 847499-27-8

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10 mM * 1 mL in DMSO ￥1278 In-stock
5 mg ￥1162 In-stock
50 mg ￥7348 In-stock
100 mg ￥8928 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities[1].

IC50 & Target

IC50: 3.8 nM (Chymotrypsin-like activity of the proteasome)[1]
体外研究
(In Vitro)

Delanzomib (CEP-18770; 20 nM; 12-24 hours) treatment results in a progressive appearance of cleaved caspases-3, -7, and -9 between 12 and 24 hours’exposure in the human MM cell lines, RPMI-8226, and U266[1].
Delanzomib (CEP-18770; 5-40 nM; 4-24 hours) treatment induces an accumulation of ubiquitinated proteins over 4 to 8 hours[1].
Delanzomib (CEP-18770) inhibits endothelial cell survival, vasculogenesis, and osteoclastogenesis in vitro; and displays a favorable cytotoxicity profile toward normal cells[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: RPMI-8226, U266, and K562 cells
Concentration: 20 nM
Incubation Time: 12 hours, 24 hours
Result: Resulted in a progressive appearance of cleaved caspases-3, -7, and -9 between 12 and 24 hours’exposure in the human MM cell lines.

Western Blot Analysis[1]

Cell Line: RPMI-8226, U266, and K562 cells
Concentration: 5 nM, 10 nM, 20 nM, 40 nM
Incubation Time: 4 hours, 8 hours, 12 hours, 24 hours
Result: Induced an accumulation of ubiquitinated proteins over 4 to 8 hours.

体内研究
(In Vivo)

Delanzomib (CEP-18770; 7.8-13 mg/kg; oral administration; twice a week; for 4 weeks) treatment results in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues, complete tumor regression of multiple myeloma (MM) xenografts and improves overall median survival in a systemic model of human MM[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 injected with RPMI 8226 cells[1]
Dosage: 7.8 mg/kg, 10 mg/kg, 13 mg/kg
Administration: Oral administration; twice a week; for 4 weeks
Result: Resulted in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues.

Clinical Trial

分子量

413.28

Formula

C21H28BN3O5
CAS 号

847499-27-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (241.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4197 mL 12.0983 mL 24.1967 mL
5 mM 0.4839 mL 2.4197 mL 4.8393 mL
10 mM 0.2420 mL 1.2098 mL 2.4197 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。-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: ≥ 2.17 mg/mL (5.25 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.25 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 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: 2.17 mg/mL (5.25 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.17 mg/mL (5.25 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 21.7 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: ≥ 2.17 mg/mL (5.25 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.25 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 21.7 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]. Piva R, et al. CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib. Blood. 2008 Mar 1;111(5):2765-75.

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Lestaurtinib(Synonyms: CEP-701; KT-5555)

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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。

Lestaurtinib (Synonyms: CEP-701; KT-5555) 纯度: 99.92%

Lestaurtinib (CEP-701;KT-5555) 是一种 ATP 竞争性的多激酶抑制剂，对 Trk 受体酪氨酸激酶家族具有强大的活性。 Lestaurtinib 抑制 JAK2，FLT3 和 TrkA 的 IC50 分别为 0.9，3，小于 25 nM。

Lestaurtinib(Synonyms: CEP-701; KT-5555)

Lestaurtinib Chemical Structure

CAS No. : 111358-88-4

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5 mg ￥7800 In-stock
10 mg   询价  
50 mg   询价  

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生物活性

Lestaurtinib (CEP-701;KT-5555) is an ATP-competitive multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.

IC50 & Target[1]

JAK2

0.9 nM (IC50)

TrkA

25 nM (IC50)

FLT3

3 nM (IC50)

Clinical Trial

分子量

439.46

Formula

C26H21N3O4
CAS 号

111358-88-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (113.78 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2755 mL 11.3776 mL 22.7552 mL
5 mM 0.4551 mL 2.2755 mL 4.5510 mL
10 mM 0.2276 mL 1.1378 mL 2.2755 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 (protect from 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：

——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    90% corn oil

    Solubility: 2.5 mg/mL (5.69 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (5.69 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.73 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

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.73 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]. Miknyoczki SJ, et al. The novel Trk receptor tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits antitumor efficacy against human pancreatic carcinoma (Panc1) xenograft growth and in vivo invasiveness. Ann N Y Acad Sci. 1999 Jun 30;880:252-62.

    [2]. Jatiani SS, et al. A Non-ATP-Competitive Dual Inhibitor of JAK2 and BCR-ABL Kinases: Elucidation of a Novel Therapeutic Spectrum Based on Substrate Competitive Inhibition. Genes Cancer. 2010;1(4):331-345.

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CEP-40783(Synonyms: RXDX-106)

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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。

CEP-40783 (Synonyms: RXDX-106) 纯度: 99.22%

CEP-40783是高效选择性，有口服活性的AXL和c-Met抑制剂，IC50值分别为7 nM 和12 nM。

CEP-40783(Synonyms: RXDX-106)

CEP-40783 Chemical Structure

CAS No. : 1437321-24-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥900 In-stock
10 mg ￥1500 In-stock
25 mg ￥3500 In-stock
50 mg ￥4500 In-stock
100 mg ￥6500 In-stock
200 mg ￥9500 In-stock
500 mg ￥17500 In-stock
1 g ￥26500 In-stock
5 g   询价  
10 g   询价  

* Please select Quantity before adding items.

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  • Anti-Cancer Compound Library
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  • Orally Active Compound Library
  • Anti-Lung Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.

IC50 & Target

IC50: 7 nM (AXL) and 12 nM (c-Met)[1]
体外研究
(In Vitro)

In AXL-transfected 293GT cells, CEP-40783 is 27-fold more active compared to recombinant enzyme with an IC50 value of 0.26 nM. CEP-40783 also demonstrates superior activity against c-Met in GTL-16 cells (IC50=6 nM). The increased inhibitory activity of CEP-40783 in cells could be attributed to its extended residence time on both AXL and c-Met, consistent with a Type II mechanism. CEP-40783 shows high kinome selectivity against 298 kinases with an S90 of 0.04 (fraction of kinases showing >90% inhibition at 1 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.
体内研究
(In Vivo)

CEP-40783 shows dose- and time-dependent inhibition of AXL phosphorylation using NCI-H1299 NSCL xenografts with 80% target inhibition at 0.3 mg/kg 6 h post dose and complete target inhibition to >90% inhibition at 1 mg/kg between 6-24 h, while a 10 mg/kg po dose resulted in complete AXL inhibition up to 48 h post dosing[1]. In 3/5 (60%) of the tumor models, CEP-40783 shows in vivo efficacy, including tumor regressions, significantly superior to that achieved with an optimal regimen of paclitaxel. In 4/4 (100%) of the erlotinib-insensitive tumor models, CEP-40783 demonstrates significant efficacy (66 to 118% TGI) compared to the control group at the 30 mg/kg dose. Additionally, CEP-40783 in combination with erlotinib demonstrate superior anti-tumor efficacy compared to CEP-40783 and erlotinib single agents in the one erlotinib-sensitive model evaluated. CEP-40783 as a single agent and in combination with erlotinib are well tolerated[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

588.56

Formula

C31H26F2N4O6
CAS 号

1437321-24-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 3.12 mg/mL (5.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6991 mL 8.4953 mL 16.9906 mL
5 mM 0.3398 mL 1.6991 mL 3.3981 mL
10 mM — — —

*

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。-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]. Sheila M, et al. CEP-40783: A potent and selective AXL/c-Met inhibitor for use in breast, non-small cell lung (NSCLC), and pancreatic cancers. [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2013 Oct 19-23; Boston, MA. Philadelphia (PA): AACR; Mol Cancer Ther 2013;12(11 Suppl):Abstract nr C275.

    [2]. Jay F, et al. Antitumor activity of the dual AXL/c-Met inhibitor CEP-40783 in Champions primary TumorGraft? models of human non-small cell lung cancer (NSCLC). [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2013 Oct 19-23; Boston, MA. Philadelphia (PA): AACR; Mol Cancer Ther 2013;12(11 Suppl):Abstract nr C272.
Animal Administration
[2]

Mice: Mice bearing established Champions TumorGrafts are treated orally with 10 mg/kg and 30 mg/kg qd of CEP-40783 for 10 to 34 days and anti-tumor efficacy and tolerability are evaluated[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]. Sheila M, et al. CEP-40783: A potent and selective AXL/c-Met inhibitor for use in breast, non-small cell lung (NSCLC), and pancreatic cancers. [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2013 Oct 19-23; Boston, MA. Philadelphia (PA): AACR; Mol Cancer Ther 2013;12(11 Suppl):Abstract nr C275.

    [2]. Jay F, et al. Antitumor activity of the dual AXL/c-Met inhibitor CEP-40783 in Champions primary TumorGraft? models of human non-small cell lung cancer (NSCLC). [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2013 Oct 19-23; Boston, MA. Philadelphia (PA): AACR; Mol Cancer Ther 2013;12(11 Suppl):Abstract nr C272.

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CEP-28122

发表于由

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。

CEP-28122 

CEP-28122是一种高度有效的选择性ALK抑制剂, IC50值为1.9 ± 0.5 nM。

CEP-28122

CEP-28122 Chemical Structure

CAS No. : 1022958-60-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CEP-28122 的其他形式现货产品:

CEP-28122 mesylate salt

生物活性

CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay. IC50 value: 1.9 ± 0.5 nM Target: ALK in vitro: CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 with IC50 of 46 ±10 nM. CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells. [1] in vivo: CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher. [1]

分子量

539.07

Formula

C28H35ClN6O3
CAS 号

1022958-60-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Cheng M, et al. CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2012 Mar;11(3):670-679.

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Agerafenib(Synonyms: CEP-32496; RXDX-105)

发表于由

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。

Agerafenib (Synonyms: CEP-32496; RXDX-105) 纯度: 99.53%

Agerafenib (CEP-32496; RXDX-105) 是一种口服高效的 BRAFV600E 抑制剂，Kd 为 14 nM。

Agerafenib(Synonyms: CEP-32496; RXDX-105)

Agerafenib Chemical Structure

CAS No. : 1188910-76-0

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1651 In-stock
5 mg ￥1450 In-stock
10 mg ￥2450 In-stock
50 mg ￥7450 In-stock
100 mg ￥9950 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.

IC50 & Target[1]

Braf

36 nM (Kd)

CRAF

39 nM (Kd)

BRafV600E

14 nM (Kd)

c-Kit

2 nM (Kd)

Ret

2 nM (Kd)

LCK

2 nM (Kd)

Abl-1

3 nM (Kd)

VEGFR-2

8 nM (Kd)

CSF-1R

9 nM (Kd)

EPHA2

14 nM (Kd)

EGFR

22 nM (Kd)

c-Met

513 nM (Kd)

JAK-2

4700 nM (Kd)

MEK-1

7100 nM (Kd)

MEK-2

8300 nM (Kd)

体外研究
(In Vitro)

Agerafenib (CEP-32496) exhibits high potency against several BRAFV600E-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAFV600E versus those containing wild-type BRAF. Agerafenib exhibits potent binding (BRAFV600E Kd=14 nM) and cellular activity (pMEK IC50=82 nM and A375 proliferation IC50=78 nM), with activity in the proliferation assay. Agerafenib also exhibits a favorable CYP450 inhibition profile, with measured IC50 values greater than 10 μM versus the CYP1A2, CYP2C9, CYP2D6, and CYP3A4 isoforms and an IC50=3.4 μM versus CYP2C19[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)

Oral administration of Agerafenib (CEP-32496) to Colo-205 tumor xenograft-bearing mice results in significant inhibition of pMEK in tumor cell lysates. For instance, a single 30 mg/kg (po) dose of Agerafenib leads to a 50 and 75% inhibition of normalized pMEK in tumor lysates at the 2 and 6 h postdose time point, respectively (p<0.03), while a 55 mg/kg (po) dose resulted in a 75% to 57% (p<0.03) inhibition of pMEK at 2 through 10 h post administration, with normalization to baseline by 24 h. Agerafenib exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib to beagle dogs (single dose of 1 mg/kg iv and 10 mg/kg po) results in low clearance (CL=5.0 (mL/min)/kg) and excellent bioavailability (%F=100). Similarly, in cynomolgus monkey, the administration of Agerafenib (single dose of 1 mg/kg iv and 10 mg/kg po) leads to high oral exposure due to low clearance (CL=6.7 mL/min/kg) and excellent bioavailability (%F=100)[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

517.46

Formula

C24H22F3N5O5
CAS 号

1188910-76-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (96.63 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9325 mL 9.6626 mL 19.3252 mL
5 mM 0.3865 mL 1.9325 mL 3.8650 mL
10 mM 0.1933 mL 0.9663 mL 1.9325 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。-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: ≥ 2.5 mg/mL (4.83 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.83 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 (4.83 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.83 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 (4.83 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.83 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]. Rowbottom MW, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.
Cell Assay
[1]

A375 cells are seeded at 10,000 cells per well in DMEM with 10% fetal calf serum and allowed to attach. The cells are washed with PBS and switched to DMEM with 0.5% of serum and incubated overnight. The test compounds (e.g., Agerafenib; 10 μM) are then added at various concentrations with a final DMSO concentration of 0.5% and incubated for 72 h. At the end of incubation, a Cell Titer Blue is added per instructions, and incubation is continued for 3 h. Remaining viable cells are quantified by measuring the strength of the fluorescence signal using SoftMax Pro (excitation at 560 nm and emission at 590 nm). IC50 values are derived using a 9-point curve and are presented as mean values from experiments performed in duplicate[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]
Six to eight week old athymic nu/nu nude mice (20-25 g) are inoculated subcutaneously with Colo-205 tumor cells (1×106/mouse) in the right flank. Upon reaching an average tumor volume of 150-200 mm3 (10-12 days post implantation), animals are randomized into treatment groups (n=10 mice/group). Each group is dosed orally for 14 days with either vehicle only (22% HPβCD) or with Agerafenib at 10, 30, or 100 mg/kg twice daily (BID), and each dose of drug is given in a volume of 0.1 mL per 20 g of body weight, adjusted for the body weight of the animal. Tumor volumes are measured three times weekly using vernier calipers, and volumes are calculated[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]. Rowbottom MW, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

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CEP-37440

发表于由

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。

CEP-37440  纯度: 99.97%

CEP-37440是新型FAK和ALK双重抑制剂，IC50分别为2.3 nM和120 nM。

CEP-37440

CEP-37440 Chemical Structure

CAS No. : 1391712-60-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1149 In-stock
5 mg ￥900 In-stock
10 mg ￥1600 In-stock
50 mg ￥6300 In-stock
100 mg ￥10230 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CEP-37440 相关产品

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  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
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  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library

生物活性

CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma). IC50 value: 2.3 nM (FAK); 120 nM (ALK cellular IC50 in 75% human plasma) Target: Dual FAK/ALK Preparation of fused bicyclic 2,4-diaminopyrimidine derivatives as a dual ALK and FAK inhibitor By Jacobs, Martin J.; Ott, Gregory R. From PCT Int. Appl. (2013), WO 2013134353 A1 20130912.

Clinical Trial

分子量

580.12

Formula

C30H38ClN7O3
CAS 号

1391712-60-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (172.38 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7238 mL 8.6189 mL 17.2378 mL
5 mM 0.3448 mL 1.7238 mL 3.4476 mL
10 mM 0.1724 mL 0.8619 mL 1.7238 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。-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: ≥ 2.5 mg/mL (4.31 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.31 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 (4.31 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.31 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 (4.31 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.31 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]. From PCT Int. Appl. (2013), WO 2013134353 A1 20130912.

    [2]. Salem I, et al. The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells. Breast Cancer Res. 2016 Mar 24;18(1):37.

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

CEP-33779

发表于由

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。

CEP-33779  纯度: 99.36%

CEP-33779是一个新颖的，选择性，有口服活性的JAK2抑制剂，IC50值为1.8±0.6 nM。

CEP-33779

CEP-33779 Chemical Structure

CAS No. : 1257704-57-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1650 In-stock
5 mg ￥1500 In-stock
10 mg ￥2200 In-stock
50 mg ￥7600 In-stock
100 mg ￥11000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CEP-33779 相关产品

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  • Kinase Inhibitor Library
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  • Differentiation Inducing Compound Library
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  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
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  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Anti-Liver Cancer Compound Library

生物活性

CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.

IC50 & Target[1]

JAK2

1.8 nM (IC50)

JAK3

150 nM (IC50)

体外研究
(In Vitro)

CEP-33779, at nontoxic concentrations, significantly sensitizes overexpression of P-glycoprotein overexpressing multidrug resistance cells to its anticancer substrates. CEP-33779 significantly increases intracellular accumulation and decreases the efflux of doxorubicin by inhibiting the overexpression of P-glycoprotein transport function[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)

CEP-33779 exhibits a favorable PK profile in nude mice, an iv half-life of 1 h, moderate distribution (Vd=2.6 L/kg), and measurable oral exposure with an estimated bioavailability of 33%. It demonstrates antitumor efficacy in the CWR22 xenograft model; oral dosing for 14 days at 30 mg/kg bid results in tumor stasis and partial regressions in 5/10 animals[1]. CEP-33779 administration results in an almost complete shrinkage of tumors in most animals; few remaining tumor nodules were small, poorly vascularized, and had a necrotic appearance. CEP-33779 suppressed activation of NF-κB in tumors[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.
分子量

462.57

Formula

C24H26N6O2S
CAS 号

1257704-57-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (108.09 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1618 mL 10.8092 mL 21.6183 mL
5 mM 0.4324 mL 2.1618 mL 4.3237 mL
10 mM 0.2162 mL 1.0809 mL 2.1618 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。-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: ≥ 2.5 mg/mL (5.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.40 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 (5.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.40 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 (5.40 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.40 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]. Dugan BJ, et al. A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. J Med Chem. 2012 Jun 14;55(11):5243-54.

    [2]. Seavey MM, et al. Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Mol Cancer Ther. 2012 Apr;11(4):984-93.

    [3]. Tang SJ, et al. CEP-33779 antagonizes ATP-binding cassette subfamily B member 1 mediated multidrug resistance by inhibiting its transport function. Biochem Pharmacol. 2014 Sep 15;91(2):144-56.

Kinase Assay
[1]

The kinase activity of baculovirus-expressed human JAK1, JAK2, or JAK3 is measured. Each 96-well Costar high binding plate is coated with 100 μL/well of 10 μg/mL neutravidin in TBS at 37 °C for 2 h, followed by 100 μL/well of 1 μg/mL 15-mer peptide substrate at 37 °C for 1 h. The kinase assay mixture (total volume=100 μL/well) consisting of 20 mM HEPES (pH 7.2), ATP (0.2 μM ATP for JAK1 and JAK2 and 0.1 μM ATP for JAK3), 1 mM MnCl2, 0.1% BSA, and CEP-33779 (diluted in DMSO, 2.5% DMSO final in assay) is added to the assay plate. Enzyme is added and the reaction is allowed to proceed for 20 min at room temperature. Detection of the phosphorylated product is performed by adding 100 μL/well of diluted Eu-N1 labeled PY100 antibody. Samples are incubated at RT for 1 h, followed by addition of 100 μL enhancement solution. Plates are agitated for 10 min, and the fluorescence of the resulting solution is measured. IC50 values are determined[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: Nude mice bearing CWR22 xenografts are dosed orally with 55 mg/kg of CEP-33779 or a vehicle (PEG400). At 2, 6, and 24 h after dosing animals (3/group) are sacrificed, tumors are excised and plasma samples are prepared. Tumor extracts are prepared using Triton-based extraction buffer supplemented with inhibitors of proteases and phosphatases. Equal amounts of extracts are resolved on SDS-PAGE gels and STAT3 phosphorylation and expression are analyzed by Western blot using specific antibodies[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]. Dugan BJ, et al. A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. J Med Chem. 2012 Jun 14;55(11):5243-54.

    [2]. Seavey MM, et al. Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Mol Cancer Ther. 2012 Apr;11(4):984-93.

    [3]. Tang SJ, et al. CEP-33779 antagonizes ATP-binding cassette subfamily B member 1 mediated multidrug resistance by inhibiting its transport function. Biochem Pharmacol. 2014 Sep 15;91(2):144-56.

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

CEP-28122 mesylate salt

发表于由

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。

CEP-28122 mesylate salt  纯度: 99.85%

CEP-28122 mesylate salt 是一种二氨基嘧啶衍生物，是一种高度有效的选择性且具有口服活性的 ALK 抑制剂，对重组 ALK 激酶活性的 IC50 为 1.9 nM。CEP-28122 在人类癌症的 ALK 阳性实验模型中具有抗肿瘤活性。 CEP-28122 具有良好的药效药代活性。

CEP-28122 mesylate salt

CEP-28122 mesylate salt Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2096 In-stock
5 mg ￥1500 In-stock
10 mg ￥2400 In-stock
50 mg ￥5500 In-stock
100 mg ￥10000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CEP-28122 mesylate salt 相关产品

•相关化合物库:

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  • Targeted Diversity Library

生物活性

CEP-28122 mesylate salt, a diaminopyrimidine derivative, is a potent, selective, and orally bioavailable ALK inhibitor, with an IC50 value of 1.9 nM for recombinant ALK kinase activity. CEP-28122 has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate salt has good pharmacodynamic and pharmacokinetic activity[1].

体外研究
(In Vitro)

CEP-28122 mesylate salt (3-3000 nM; 48 hours) treatment leads to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture, associates with concentration-related caspase 3/7 activation[1].
CEP-28122 mesylate salt (30-1000 nM; 2 hours) treatment leads to substantial suppression of phosphorylation of putative downstream effectors of ALK in Sup-M2 cells, indicating that the downstream signaling pathways are mediated by individual ALK fusion protein[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 Cytotoxicity Assay[1]

Cell Line: Karpas-299, Sup-M2, Toledo and HuT-102 cells
Concentration: 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time: 48 hours
Result: Treatment led to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture.

Western Blot Analysis [1]

Cell Line: Sup-M2 cells
Concentration: 30 nM, 100 nM, 300 nM, 1000 nM
Incubation Time: 2 hours
Result: Resulted in substantial suppression of phosphorylation of putative downstream effectors of ALK, including Stat-3, Akt, and ERK1/2 in Sup-M2 cells.

体内研究
(In Vivo)

CEP-28122 mesylate salt (3-30 mg/kg; oral gavage; twice a day; 12 days) produces dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice.In contrast, CEP-28122 has no antitumor activity in nu/nu mice bearing HCT116, suggesting that the antitumor activity of CEP-28122 in NPM-ALK–positive Sup-M2 tumor models is due to sustained NPM-ALK inhibition in tumors [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: Female SCID mice bearing Sup-M2 subcutaneous tumor xenografts and nu/nu mice bearing HCT116 aged 6-8 week old[1]
Dosage: 3 mg/kg, 10 mg/kg and 30 mg/kg
Administration: oral gavage; twice a day; 12 days
Result: CEP-28122 produced dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice. In contrast, CEP-28122 had no antitumor activity in nu/nu mice bearing HCT116.

分子量

635.17

Formula

C29H39ClN6O6S
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 : ≥ 6.4 mg/mL (10.08 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 1.5744 mL 7.8719 mL 15.7438 mL
5 mM 0.3149 mL 1.5744 mL 3.1488 mL
10 mM 0.1574 mL 0.7872 mL 1.5744 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。
参考文献

  • [1]. Mangeng Cheng, et al. CEP-28122, a highly potent and selective orally active inhibitor of anaplastic lymphoma kinase with antitumor activity in experimental models of human cancers. Mol Cancer Ther. 2012 Mar;11(3):670-9.

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

CEP-9722

发表于由

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。

CEP-9722 

CEP-9722 是 CEP-8983 的前药，是一种选择性且具有口服活性的PARP-1 和 PARP-2 抑制剂，IC50 分别为 20 nM 和 6 nM。CEP-9722 具有抗癌作用。

CEP-9722

CEP-9722 Chemical Structure

CAS No. : 916574-83-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CEP-9722, the prodrug of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects[1][2].

IC50 & Target[2]

PARP-1

20 nM (IC50)

PARP-2

6 nM (IC50)

体内研究
(In Vivo)

CEP-9722 (100-200 mg/kg/day; oral gavage; once daily; for 5 days a week for 4 weeks) shows dose-dependent antitumor activity in RT4 xenografts; 200 mg/kg daily is better than control and 100 mg/kg is not[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice bearing subcutaneous RT4 human urothelial carcinoma (UC) tumors[1]
Dosage: 100 or 200 mg/kg/day
Administration: Oral gavage; once daily; for 5 days a week for 4 weeks
Result: Showed dose-dependent antitumor activity in RT4 xenografts.

分子量

418.49

Formula

C24H26N4O3
CAS 号

916574-83-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Weiguo Jian, et al. Activity of CEP-9722, a poly (ADP-ribose) polymerase inhibitor, in urothelial carcinoma correlates inversely with homologous recombination repair response to DNA damage. Anticancer Drugs. 2014 Sep;25(8):878-86.

    [2]. Ruth Plummer, et al. Phase 1 dose-escalation study of the PARP inhibitor CEP-9722 as monotherapy or in combination with temozolomide in patients with solid tumors. Cancer Chemother Pharmacol. 2014 Aug;74(2):257-65.

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

CEP-9722

发表于由

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。

CEP-9722 

CEP-9722 是 CEP-8983 的前药，是一种选择性且具有口服活性的PARP-1 和 PARP-2 抑制剂，IC50 分别为 20 nM 和 6 nM。CEP-9722 具有抗癌作用。

CEP-9722

CEP-9722 Chemical Structure

CAS No. : 916574-83-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CEP-9722, the prodrug of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects[1][2].

IC50 & Target[2]

PARP-1

20 nM (IC50)

PARP-2

6 nM (IC50)

体内研究
(In Vivo)

CEP-9722 (100-200 mg/kg/day; oral gavage; once daily; for 5 days a week for 4 weeks) shows dose-dependent antitumor activity in RT4 xenografts; 200 mg/kg daily is better than control and 100 mg/kg is not[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice bearing subcutaneous RT4 human urothelial carcinoma (UC) tumors[1]
Dosage: 100 or 200 mg/kg/day
Administration: Oral gavage; once daily; for 5 days a week for 4 weeks
Result: Showed dose-dependent antitumor activity in RT4 xenografts.

分子量

418.49

Formula

C24H26N4O3
CAS 号

916574-83-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Weiguo Jian, et al. Activity of CEP-9722, a poly (ADP-ribose) polymerase inhibitor, in urothelial carcinoma correlates inversely with homologous recombination repair response to DNA damage. Anticancer Drugs. 2014 Sep;25(8):878-86.

    [2]. Ruth Plummer, et al. Phase 1 dose-escalation study of the PARP inhibitor CEP-9722 as monotherapy or in combination with temozolomide in patients with solid tumors. Cancer Chemother Pharmacol. 2014 Aug;74(2):257-65.

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

CEP-9722

发表于由

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。

CEP-9722 

CEP-9722 是 CEP-8983 的前药，是一种选择性且具有口服活性的PARP-1 和 PARP-2 抑制剂，IC50 分别为 20 nM 和 6 nM。CEP-9722 具有抗癌作用。

CEP-9722

CEP-9722 Chemical Structure

CAS No. : 916574-83-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CEP-9722, the prodrug of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC50s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects[1][2].

IC50 & Target[2]

PARP-1

20 nM (IC50)

PARP-2

6 nM (IC50)

体内研究
(In Vivo)

CEP-9722 (100-200 mg/kg/day; oral gavage; once daily; for 5 days a week for 4 weeks) shows dose-dependent antitumor activity in RT4 xenografts; 200 mg/kg daily is better than control and 100 mg/kg is not[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 bearing subcutaneous RT4 human urothelial carcinoma (UC) tumors[1]
Dosage: 100 or 200 mg/kg/day
Administration: Oral gavage; once daily; for 5 days a week for 4 weeks
Result: Showed dose-dependent antitumor activity in RT4 xenografts.

分子量

418.49

Formula

C24H26N4O3
CAS 号

916574-83-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Weiguo Jian, et al. Activity of CEP-9722, a poly (ADP-ribose) polymerase inhibitor, in urothelial carcinoma correlates inversely with homologous recombination repair response to DNA damage. Anticancer Drugs. 2014 Sep;25(8):878-86.

    [2]. Ruth Plummer, et al. Phase 1 dose-escalation study of the PARP inhibitor CEP-9722 as monotherapy or in combination with temozolomide in patients with solid tumors. Cancer Chemother Pharmacol. 2014 Aug;74(2):257-65.

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