SAR-020106

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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。

SAR-020106  纯度: 98.53%

SAR-020106 是一种 ATP 竞争性的、选择性好的 CHK1 抑制剂，IC50 为 13.3 nM。SAR-020106 对 CHK2 具有良好的选择性。SAR-020106 在几种结肠肿瘤细胞系中以 p53 依赖性方式将 Gemcitabine 和 SN38 的细胞杀伤力提高了 3.0 到 29 倍。SAR-020106 可通过选择抗癌药物增强抗肿瘤活性。

SAR-020106

SAR-020106 Chemical Structure

CAS No. : 1184843-57-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2200 In-stock
5 mg ￥2000 In-stock
10 mg ￥3200 In-stock
25 mg ￥6000 In-stock
50 mg ￥9500 In-stock
100 mg   询价  
200 mg   询价  

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SAR-020106 相关产品

•相关化合物库:

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

生物活性

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer drugs[1][2].

IC50 & Target[1]

Chk1

13.3 nM (IC50)

体外研究
(In Vitro)

SAR-020106 (0.1-1 μM; 23 hours) abrogates an Etoposide-induced S and G2 arrest[1].
SAR-020106 is capable of abrogating Etoposide-induced cell cycle arrest with an IC50 of 55 nM and 91 nM in HT29 and SW620 cells, respectively. SAR-020106 is relatively nontoxic with a GI50 of 0.48 μM in HT29 and 2 μM in SW620, resulting in an activity index of 8.7 and 22, respectively. SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion[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)

SAR-020106 (40 mg/kg; i.p.; administered on days 0, 1, 7, 8, 14, and 15) in combination with Irinotecan potentiates the antitumor activity in SW620 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: Nude mice bearing SW620 xenograft tumors[1]
Dosage: 40 mg/kg
Administration: I.p.; administered on days 0, 1, 7, 8, 14, and 15
Result: There was a clear decrease in tumor growth associated with the combination with tumors reaching 300% by 12.5 days.

分子量

382.85

Formula

C19H19ClN6O
CAS 号

1184843-57-9
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 : 5 mg/mL (13.06 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6120 mL 13.0599 mL 26.1199 mL
5 mM 0.5224 mL 2.6120 mL 5.2240 mL
10 mM 0.2612 mL 1.3060 mL 2.6120 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。
参考文献

  • [1]. Walton MI, et al. The preclinical pharmacology and therapeutic activity of the novel CHK1 inhibitor SAR-020106. Mol Cancer Ther. 2010;9(1):89-100.

    [2]. Reader JC, et al. Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem. 2011;54(24):8328-8342.

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