标签归档：tartrate

Catharanthine Tartrate(Synonyms: 酒石酸长春质碱; (+)-3,4-Didehydrocoronaridine Tartrate)

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。

Catharanthine Tartrate (Synonyms: 酒石酸长春质碱; (+)-3,4-Didehydrocoronaridine Tartrate) 纯度: 99.92%

Catharanthine Tartrate 是长春花中的生物碱类物质，抑制电压门控 L 型钙离子通道 (voltage-operated L-type Ca2+ channel)，具有抗肿瘤、降血压的活性。

Catharanthine Tartrate(Synonyms: 酒石酸长春质碱; (+)-3,4-Didehydrocoronaridine Tartrate)

Catharanthine Tartrate Chemical Structure

CAS No. : 4168-17-6

规格 价格 是否有货 数量
5 mg ￥600 In-stock
10 mg ￥1000 In-stock
50 mg ￥3500 In-stock
100 mg   询价  
200 mg   询价  

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  • Neuroprotective Compound Library
  • Alkaloids Library

生物活性

Catharanthine Tartrate is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca2+ channel, with anti-cancer and blood pressure-lowering activity[1].

分子量

486.51

Formula

C25H30N2O8
CAS 号

4168-17-6
中文名称

酒石酸长春质碱；长春质碱酒石酸盐
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 : 100 mg/mL (205.55 mM; Need ultrasonic)

H2O : 5 mg/mL (10.28 mM; ultrasonic and warming and adjust pH to 3 with HCl 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 2.0555 mL 10.2773 mL 20.5546 mL
5 mM 0.4111 mL 2.0555 mL 4.1109 mL
10 mM 0.2055 mL 1.0277 mL 2.0555 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：

——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 (5.14 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.14 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 (5.14 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.14 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 (5.14 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.14 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 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Jadhav A, et al. Catharanthine dilates small mesenteric arteries and decreases heart rate and cardiac contractility by inhibition of voltage-operated calcium channels on vascular smooth muscle cells and cardiomyocytes. J Pharmacol Exp Ther. 2013 Jun;345(3):383-92.

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Giredestrant tartrate(Synonyms: GDC-9545 tartrate)

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。

Giredestrant tartrate (Synonyms: GDC-9545 tartrate)

Giredestrant tartrate (GDC-9545 tartrate)，一种非甾体 ER 配体，也是一种口服有效的，选择性雌激素受体 (ER) 拮抗剂。Giredestrant tartrate 可以在 ER 配体结合域内与雌二醇竞争结合并诱导构象变化。Giredestrant tartrate 具有抗肿瘤活性。

Giredestrant tartrate(Synonyms: GDC-9545 tartrate)

Giredestrant tartrate Chemical Structure

CAS No. : 2407529-33-1

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

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Giredestrant tartrate 的其他形式现货产品:

Giredestrant

生物活性

Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity[1].

IC50 & Target[1]

Estrogen receptor

 

体外研究
(In Vitro)

Giredestrant (GDC-9545) tartrate consistently induces ER turnover and drives deep transcriptional suppression of ER, resulting in robust in vitro anti-proliferative activity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Giredestrant (GDC-9545) tartrate is an ER antagonist that combines desirable mechanistic and pre-clinical DMPK attributes. The highly potent in vivo efficacy of Giredestrant likely arises due to the particular combination of high binding potency, full suppression of ER signaling, and an improved DMPK profile[1].

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

分子量

672.64

Formula

C31H37F5N4O7
CAS 号

2407529-33-1
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]. C Metcalfe, et al. Abstract P5-04-07: GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes.

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ENMD-2076 Tartrate

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。

ENMD-2076 Tartrate  纯度: 98.87%

ENMD-2076 Tartrate 是多靶点激酶抑制剂，抑制 Aurora A，Flt3，KDR/VEGFR2，Flt4/VEGFR3，FGFR1，FGFR2，Src，PDGFRα 的IC50 值分别为1.86，14，58.2，15.9，92.7，70.8，20.2 and 56.4 nM。

ENMD-2076 Tartrate

ENMD-2076 Tartrate Chemical Structure

CAS No. : 1291074-87-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1390 In-stock
5 mg ￥1200 In-stock
10 mg ￥1800 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

IC50 & Target[1]

Aurora A

1.86 nM (IC50)

KDR

58.2 nM (IC50)

Flt-4

15.9 nM (IC50)

FGFR1

92.7 nM (IC50)

FGFR2

70.8 nM (IC50)

PDGFRα

56.4 nM (IC50)

Flt3

14 nM (IC50)

体外研究
(In Vitro)

ENMD-2076 is selective toward Aurora A versus Aurora B (IC50=350 nM). ENMD-2076 inhibits HUVEC growth with an IC50 value of 0.15 mM. Against 10 human leukemia cell lines, the IC50 values range from 0.025 to 0.53 mM. Within this panel, MV4:11 cells are the most sensitive cells by a factor of greater than 4. The lymphoma-derived U937 cell line treated with ENMD-2076 shows that the ENMD-2076 induces a dose-dependent increase in G2-M-phase arrest as well as the induction of apoptosis. ENMD-2076 inhibits cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation in THP-1 cells, which have been shown to express FL-responsive wild-type Flt- 3 (18) with an IC50 value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC50 value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC50 value of 7 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)

ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model[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

525.56

Formula

C25H31N7O6
CAS 号

1291074-87-7
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 : 25 mg/mL (47.57 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9027 mL 9.5137 mL 19.0273 mL
5 mM 0.3805 mL 1.9027 mL 3.8055 mL
10 mM 0.1903 mL 0.9514 mL 1.9027 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: ≥ 1.43 mg/mL (2.72 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (2.72 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 14.3 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: ≥ 1.43 mg/mL (2.72 mM); Clear solution

    此方案可获得 ≥ 1.43 mg/mL (2.72 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 14.3 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]. Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37.

    [2]. Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25.
Kinase Assay
[1]

Recombinant Aurora A and B kinase enzymes assays are carried out in kinase assay buffer (50 mM of HEPES, pH 7.5, 10 mM of MgCl2, 5 mM of EGTA, 0.05% Brij-35) supplemented with 2 mM of DTT. Activities are determined at an ATP concentration equivalent to the apparent Km for each enzyme, and an enzyme concentration that results in approximately 30% phosphorylation of the peptide substrate after 1 hour. Dose–response curves of relative enzyme activity versus ENMD-2076 concentration are plotted with Grafit and used to calculate IC50 values[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
[1]

The antiproliferative effect of ENMD-2076 on adherent tumor cell lines is measured by plating 500 cells per well in a 96-well plate and incubating with 9 doses of compound, spanning 0.3 nM to 125 mM, for 96 hours. Cellular proliferation is measured using the sulforhodamine B 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: Cell lines are injected subcutaneously or into the mammary fat pad (MDA-MB-231 only) of 5- to 6-week-old CB.17 SCID or NCr nude mice. Tumors are allowed to grow for 10 to 50 days before drug treatment. All treatments are with ENMD-2076 in water or ENMD-2076 free base in CMC-Tween vehicle (0.075% carboxymethylcellulose, 0.085% Tween 80 in water), administered orally. Percent tumor growth inhibition is 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]. Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37.

    [2]. Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25.

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Rucaparib tartrate(Synonyms: AG-014699 tartrate; PF-01367338 tartrate)

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。

Rucaparib tartrate (Synonyms: AG-014699 tartrate; PF-01367338 tartrate)

Rucaparib (AG014699) tartrate 是一种口服有效的 PARP 蛋白 (PARP-1, PARP-2 and PARP-3) 抑制剂，对 PARP-1 的 Ki 为 1.4 nM。Rucaparib tartrate 是六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib tartrate 具有用于去势抵抗性前列腺癌 (CRPC) 研究的潜力。

Rucaparib tartrate(Synonyms: AG-014699 tartrate; PF-01367338 tartrate)

Rucaparib tartrate Chemical Structure

CAS No. : 773059-22-6

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

* Please select Quantity before adding items.

Rucaparib tartrate 的其他形式现货产品:

Rucaparib

生物活性

Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].

IC50 & Target[1]

PARP-1

1.4 nM (Ki)

PARP-2

 

PARP-3

 

体外研究
(In Vitro)

Rucaparib (AG014699) tartrate is a possible N-demethylation metabolite of AG14644[1].
Rucaparib (0.1, 1, 10, 100 μM; 24 hours) tartrate is cytotoxic and has the LC50 being 5 μM in Capan-1 (BRCA2 mutant) cells and only 100 nM in MX-1 (BRCA1 mutant) cells[2].
The radio-sensitization by Rucaparib tartrate is due to downstream inhibition of activation of NF-κB, and is independent of SSB repair inhibition. Rucaparib tartrate can target NF-κB activated by DNA damage and overcome toxicity observed with classical NF-κB inhibitors without compromising other vital inflammatory functions[5].
Rucaparib tartrate inhibits PARP-1 activity by 97.1% at a concentration of 1 μM in permeabilised D283Med cells[6].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Rucaparib (AG014699) tartrate and AG14584 significantly increase Temozolomide toxicity. Rucaparib (1 mg/kg) tartrate significantly increases Temozolomide-induced body weight loss. Rucaparib (0.1 mg/kg) tartrate esults in a 50% increase in the temozolomide-induced tumor growth delay[1].
Rucaparib (10 mg/kg for i.p. or 50, 150 mg/kg for p.o.; daily for 5 days per week for 6 weeks) tartrate significantly inhibits the growth of the tumor, and there is one complete tumor regression and two persistent partial regressions[2].
Rucaparib (150 mg/kg; p.o.; once per week for 6 weeks or three times per week for 6 weeks) tartrate has greatest antitumor effect with three complete regressions[2].
Rucaparib tartrate enhances the antitumor activity of temozolomide and indicates complete and sustained tumor regression in NB1691 and SHSY5Y xenografts[6].

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

473.45

Formula

C23H24FN3O7
CAS 号

773059-22-6
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]. Thomas HD, et al. Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial. Mol Cancer Ther, 2007, 6(3), 945-956.

    [2]. J Murray, et al. Tumour cell retention of rucaparib, sustained PARP inhibition and efficacy of weekly as well as daily schedules. Br J Cancer. 2014 Apr 15;110(8):1977-84.

    [3]. Matt Shirley, et al. Rucaparib: A Review in Ovarian Cancer. Target Oncol. 2019 Apr;14(2):237-246.

    [4]. Jianneng Li, et al. Hexose-6-phosphate dehydrogenase blockade reverses prostate cancer drug resistance in xenograft models by glucocorticoid inactivation. Sci Transl Med. 2021 May 26;13(595):eabe8226.

    [5]. Hunter JE, et al. NF-κB mediates radio-sensitization by the PARP-1 inhibitor, AG-014699. Oncogene, 2012, 31(2), 251-264.

    [6]. Daniel RA, et al. Inhibition of poly(ADP-ribose) polymerase-1 enhances temozolomide and topotecan activity against childhood neuroblastoma. Clin Cancer Res, 2009, 15(4), 1241-1249.

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Tartaric acid disodium dihydrate(Synonyms: Sodium tartrate dibasic dihydrate; Sodium tartrate dihydrate)

发表于由

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Tartaric acid disodium dihydrate (Synonyms: Sodium tartrate dibasic dihydrate; Sodium tartrate dihydrate) 纯度: ≥98.0%

酒石酸钠二元二水合物是一种钠盐, 在分子生物学和细胞培养中用作缓冲液, 是酸性磷酸酶抑制剂, 增加秋水仙碱结合tubulin1率。

Tartaric acid disodium dihydrate(Synonyms: Sodium tartrate dibasic dihydrate; Sodium tartrate dihydrate)

Tartaric acid disodium dihydrate Chemical Structure

CAS No. : 6106-24-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in Water ￥550 In-stock
500 mg ￥500 In-stock
5 g ￥600 In-stock
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Tartaric acid disodium dihydrate 相关产品

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生物活性

Tartaric acid disodium dihydrate is a Acid phosphatase inhibitor, is a sodium salt used in buffers for molecular biology and cell culture applications. Increases the rate of colchicine binding to tubulin1.

分子量

232.10

Formula

C4H10Na2O8
CAS 号

6106-24-7
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: 

H2O : 100 mg/mL (430.85 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.3085 mL 21.5424 mL 43.0849 mL
5 mM 0.8617 mL 4.3085 mL 8.6170 mL
10 mM 0.4308 mL 2.1542 mL 4.3085 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。

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