CDK7-IN-8

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK7-IN-8 

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。

CDK7-IN-8

CDK7-IN-8 Chemical Structure

CAS No. : 2654003-64-0

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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[1].

IC50 & Target[1]

CDK7

54.29 nM (IC50)

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 IC50 of 50.85 nM, 45.31 nM, 25.26 nM and 44.47 nM respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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%.

分子量

498.62

Formula

C25H38N8O3
CAS 号

2654003-64-0
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.
参考文献

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

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