| 产品描述： | Chk1 选择性抑制剂;Chk1 Selective Inhibitors;产品介绍：SAR-020106是一种ATP竞争性的、选择性好的CHK1抑制剂，IC50为13.3nM。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。;InformationSAR-020106 is an ATP-competitive, potent, and selectiveCHK1inhibitor with an IC50 of 13.3 nM.TargetsChk1 (Cell-free assay) 13.3 nMIn vitroSAR-020106 abrogates an etoposide-induced G2 arrest with an IC50 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. SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion.In vivoSAR-020106 can enhance the antitumor effects of both irinotecan and gemcitabine in vivo with appropriate biomarker changes and minimal toxicity. Although having minimal oral bioavailability in mice (F = 5%), distribution of SAR-020106 following i.p. dosing (40 mg/kg) was sufficient to inhibit CHK1 in the tumors, as shown by inhibition of the irinotecan-induced CHK1 pS296 autophosphorylation. At doses giving inhibition of CHK1 activity the selective CHK1 inhibitor SAR-020106 showed no single agent activity in the SW620 xenograft model, and tumors grew at similar rates to the vehicle-treated controls. When dosed (i.p.) in combination with irinotecan, SAR-020106 was observed to potentiate the antitumor activity of the genotoxic drug in the SW620 xenograft model.Cell Research(from reference)Cell lines：SW620 colon cancer cells Concentrations：5 μM Incubation Time：24 h |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京