CDK7-IN-8 是一种有效的CDK7抑制剂，IC50为 54.29 nM。CDK7-IN-8 对一些癌细胞和体内肿瘤模型有抑制作用。
| 生物活性 | CDK7-IN-8 is a potentCDK7inhibitor withIC50of 54.29 nM. CDK7-IN-8 has inhibitory effect on certaincancercells andin vivotumor models[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | CDK7-IN-8 (0-100 nM; 72 hours) has inhibitory effect on HCC70, OVCAR-3, HCT116 and HCC1806 cells, with IC50of 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 IC50of 50.85 nM, 45.31 nM, 25.26 nM and 44.47 nM respectively. |
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体内研究
(In Vivo) | 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%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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