产品
编 号:F741053
分子式:C14H11N3O
分子量:237.26
产品类型
结构图
CAS No: 918523-75-8
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产品详情
生物活性:
CDK8-IN-13 is a potent, selective and orally active CDK8 inhibitor with an IC50 value of 51.9 nM. CDK8-IN-13 induces Apoptosis. CDK8-IN-13 decreases the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 shows antitumor activity.
体内研究:
CDK8-IN-13 (40、80 mg/kg;口服;持续 15 天) 在小鼠体内以剂量依赖性方式抑制肿瘤生长。Animal Model:6-week-old Balb/C mice (C1498 cells)
Dosage:40, 80 mg/kg
Administration:P.o.; for 15 days
Result:Decreased the tumor growth with no significant weight loss,the expression of Ki67 decreased in a dose-dependent manner, the level of phosphorylation of STAT1 S727 in tumor tissues was downregulated.
体外研究:
CDK8-IN-13 (compound 43; 1, 2.5, 5, 10 μM; 12 h) 以剂量依赖性方式降低 HCT-116 细胞中 p-STAT1 S727 和 p-STAT5 S726 的表达 .CDK8-IN-13 (0, 1, 5, 10 μM; 48 h) 以剂量依赖的方式诱导细胞凋亡。