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编 号：F756352
分子式：C24H20F3N3O
分子量：423.43
分子式：C24H20F3N3O
分子量：423.43
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CAS No: 2850253-95-9
产品详情
生物活性：
CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC50 value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies.
体内研究：
CDK8-IN-9 (compound 22) (p.o., 20, 40 and 80 mg/kg, daily, 3 weeks) significantly reduces in tumor volume and inhibits weight loss in mice at the concentration of 80 mg/kg in Balb/c mice infected with CT-26 murine colon cancer cells.Animal Model:Sprague?Dawley rats
Dosage:10 mg/kg or 5 mg/kg
Administration:p.o. for 10 mg/kg and i.v. for 5 mg/kg
Result:The pharmacokinetic parameters of CDK8-IN-9 (compound 22) Parameterst1/2 (h)Tmax (h)MRT (h)Cmax (μg/L) AUC0-∞ (μg/L·h)CL (L/h/kg) F (%)
10 mg/kg (po)1.210.752.022497.56783.669.2339.8
5 mg/kg (iv)1.63-1.756706.29983.0911.32-
体外研究：
CDK8-IN-9 (compound 22) (0-100 μM, 48 h) can significantly inhibit cell proliferation and target CDK8 to inhibit the activation of the WNT/β-catenin pathway, thereby suppressing β-catenin-mediated transcriptional activity of TCF/ LEF. CDK8-IN-9 (compound 22) (0.5,1 and 2 μM, 24 h) induces G2/M and S-phase cell cycle arrest, thereby inhibiting cell proliferation rather than inducing apoptosis.
CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC50 value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies.
体内研究：
CDK8-IN-9 (compound 22) (p.o., 20, 40 and 80 mg/kg, daily, 3 weeks) significantly reduces in tumor volume and inhibits weight loss in mice at the concentration of 80 mg/kg in Balb/c mice infected with CT-26 murine colon cancer cells.Animal Model:Sprague?Dawley rats
Dosage:10 mg/kg or 5 mg/kg
Administration:p.o. for 10 mg/kg and i.v. for 5 mg/kg
Result:The pharmacokinetic parameters of CDK8-IN-9 (compound 22) Parameterst1/2 (h)Tmax (h)MRT (h)Cmax (μg/L) AUC0-∞ (μg/L·h)CL (L/h/kg) F (%)
10 mg/kg (po)1.210.752.022497.56783.669.2339.8
5 mg/kg (iv)1.63-1.756706.29983.0911.32-
体外研究：
CDK8-IN-9 (compound 22) (0-100 μM, 48 h) can significantly inhibit cell proliferation and target CDK8 to inhibit the activation of the WNT/β-catenin pathway, thereby suppressing β-catenin-mediated transcriptional activity of TCF/ LEF. CDK8-IN-9 (compound 22) (0.5,1 and 2 μM, 24 h) induces G2/M and S-phase cell cycle arrest, thereby inhibiting cell proliferation rather than inducing apoptosis.
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