Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SAR-020106 是一种强效、ATP 竞争性和选择性 CHK1 抑制剂,IC50为 13.3 nM。它对 CHK2 具有良好的选择性,可通过选择抗癌药物增强抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 980 | 现货 | ||
10 mg | ¥ 1,570 | 现货 | ||
25 mg | ¥ 3,380 | 现货 | ||
50 mg | ¥ 4,820 | 现货 | ||
100 mg | ¥ 6,690 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,180 | 现货 |
产品描述 | SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme. |
靶点活性 | Chk1:13.3 nM (IC50) |
体外活性 | SAR-020106 potentiated the efficacies of irinotecan and gemcitabine in SW620 human colon carcinoma xenografts in nude mice[2] |
体内活性 | SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion. Biomarker studies have shown that SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion both in vitro and in vivo. Cytotoxic drug combinations were associated with increased gammaH2AX and poly ADP ribose polymerase cleavage consistent with the SAR-020106-enhanced DNA damage and tumor cell death. Irinotecan and gemcitabine antitumor activity was enhanced by SAR-020106 in vivo with minimal toxicity. SAR-020106 represents a novel class of CHK1 inhibitors that can enhance antitumor activity with selected anticancer drugs in vivo and may therefore have clinical utility[1]. |
分子量 | 382.85 |
分子式 | C19H19ClN6O |
CAS No. | 1184843-57-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12 mg/mL (31.34 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.612 mL | 13.0599 mL | 26.1199 mL | 65.2997 mL |
5 mM | 0.5224 mL | 2.612 mL | 5.224 mL | 13.0599 mL | |
10 mM | 0.2612 mL | 1.306 mL | 2.612 mL | 6.53 mL | |
20 mM | 0.1306 mL | 0.653 mL | 1.306 mL | 3.265 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SAR-020106 1184843-57-9 Cell Cycle/Checkpoint Chk SAR020106 cycle SN38 selectivity SW620 cancer inhibit colon cells SAR 020106 Checkpoint Kinase (Chk) antitumor arrest Inhibitor inhibitor