产品
编 号：F754420
分子式：C25H38N8O3
分子量：498.62
分子式：C25H38N8O3
分子量：498.62
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CAS No: 2654003-64-0
产品详情
生物活性：
CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models.
体内研究：
CDK7-IN-8 (20 or 40 mg/kg; i.g., single) has good advantages Pharmacokinetic properties.CDK7-IN-8 (25 mg/kg; p.o., qd, for 21 days) effectively inhibits tumor proliferation with tumor growth inhibition (TGI) value of 81.9%.Pharmacokinetic Parameters of CDK7-IN-8 in male ICR mice.IG (20 mg/kg) IG (40 mg/kg)
T1/2 (h)1.482.99
Tmax (h)0.504.67
Cmax (ng/mL)3379.92783.01
AUC0-t (h*ng/mL)6258.347828.87
AUC0-∞ (h*ng/mL)6375.007879.45
Animal Model:Male ICR mice
Dosage:20 or 40 mg/kg
Administration:i.g., single (pharmacokinetic analysis)
Result:Showed good advantages Pharmacokinetic properties.
Animal Model:Male BALB/c nude mice (injected with HCT116 tumor cells)
Dosage:25 mg/kg
Administration:p.o., qd, for 21 days
Result:Effectively inhibited tumor proliferation with tumor growth inhibition (TGI) value of 81.9%.
体外研究：
CDK7-IN-8 (0-100 nM; 72 hours) has inhibitory effect on HCC70, OVCAR-3, HCT116 and HCC1806 cells, with IC50 of 50.85 nM, 45.31 nM, 25.26 nM and 44.47 nM respectively.
CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models.
体内研究：
CDK7-IN-8 (20 or 40 mg/kg; i.g., single) has good advantages Pharmacokinetic properties.CDK7-IN-8 (25 mg/kg; p.o., qd, for 21 days) effectively inhibits tumor proliferation with tumor growth inhibition (TGI) value of 81.9%.Pharmacokinetic Parameters of CDK7-IN-8 in male ICR mice.IG (20 mg/kg) IG (40 mg/kg)
T1/2 (h)1.482.99
Tmax (h)0.504.67
Cmax (ng/mL)3379.92783.01
AUC0-t (h*ng/mL)6258.347828.87
AUC0-∞ (h*ng/mL)6375.007879.45
Animal Model:Male ICR mice
Dosage:20 or 40 mg/kg
Administration:i.g., single (pharmacokinetic analysis)
Result:Showed good advantages Pharmacokinetic properties.
Animal Model:Male BALB/c nude mice (injected with HCT116 tumor cells)
Dosage:25 mg/kg
Administration:p.o., qd, for 21 days
Result:Effectively inhibited tumor proliferation with tumor growth inhibition (TGI) value of 81.9%.
体外研究：
CDK7-IN-8 (0-100 nM; 72 hours) has inhibitory effect on HCC70, OVCAR-3, HCT116 and HCC1806 cells, with IC50 of 50.85 nM, 45.31 nM, 25.26 nM and 44.47 nM respectively.
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