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 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC 50 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.

Solid

Chk1 13.3 nM (IC50)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 5 mg/mL (13.06 mM; Need ultrasonic)配制储备液