• 产品描述： 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 agents

• 靶点： Chk1:13.3 nM (IC50);Chk

• 体外研究：
  SAR-020106 (0.1-1 μM; 23 hours) abrogates an Etoposide-induced S and G2 arrest.
  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.

• 体内研究：
  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 Animal Model: Nude mice bearing SW620 xenograft tumors 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.

• 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.612 ml	13.06 ml	26.12 ml
  5 mM	0.522 ml	2.612 ml	5.224 ml
  10 mM	0.261 ml	1.306 ml	2.612 ml
  50 mM	0.052 ml	0.261 ml	0.522 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *