CDK7-IN-8

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[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

CDK7:54.29 nM (IC50)

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[1]. Cell Proliferation Assay Cell Line: HCC70, OVCAR-3, HCT116 and HCC1806 cells[1] Concentration: 0-100 nM Incubation Time: 72 hours Result: Exhibited 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 (20 or 40 mg/kg; i.g., single) has good advantages Pharmacokinetic properties[1]. 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%[1]. Pharmacokinetic Parameters of CDK7-IN-8 in male ICR mice[1]. IG (20 mg/kg) IG (40 mg/kg) T1/2 (h) 1.48 2.99 Tmax (h) 0.50 4.67 Cmax (ng/mL) 3379.92 783.01 AUC0-t (h*ng/mL) 6258.34 7828.87 AUC0-∞ (h*ng/mL) 6375.00 7879.45 Animal Model: Male ICR mice [1] 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)[1] 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%.

[1]. Hu Yonghan, et al. Heterocyclic compound, and pharmaceutical composition thereof, preparation method therefor, intermediate thereof and application thereof. WO2021121390