化合物SAR-020106 T21331

Product Introduction
Bioactivity


英文名: SAR-020106

描述: 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。

体外活性: SAR-020106 在裸鼠体内增强了 SW620 人结肠癌异种移植物对伊立替康和吉西他滨的疗效[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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 12 mg/mL (31.34 mM)


关键字: SAR020106 | cycle | SN38 | selectivity | SW620 | cancer | inhibit | colon | cells | SAR-020106 | SAR 020106 | Checkpoint Kinase (Chk) | antitumor | arrest | Inhibitor

相关产品: SB-218078 | Prexasertib | 4-Demethyldeoxypodophyllotoxin | M443 | Buddlejasaponin IV | CHK1-IN-2 | BX-912 | MBM-55 | PD0166285 | CCT241533 hydrochloride

相关库: Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Anti-Cancer Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

化合物SAR-020106 T21331信息由TargetMol中国为您提供，如您想了解更多关于化合物SAR-020106 T21331报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途