包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | CDK7-IN-20 is a potent, selective and irreversibleCDK7(CDK) inhibitor with anIC50value of 4 nM. CDK7-IN-20 displays >206-fold selectivity forCDK7overCDK1,CDK2,CDK3,CDK5,CDK6,CDK9andCDK12. CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research[1]. | |||||||||||||||||||||||||||||||||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | In Madin-Darby canine kidney (MDCK) cells, CDK7-IN-20 (Compound B2; 1-3 μM; from day 4 to day 12) shows high potency to inhibit cyst growth and exhibited lower cytotoxicity than THZ1[1]. | |||||||||||||||||||||||||||||||||||||||||||||||
体内研究 (In Vivo) | CDK7-IN-20 (Compound B2; 5 mg/kg; s.c; once daily; for 6 days) significantly reduces the kidney size and cyst formation of the ADPKD mice. The protein expression of AMPD3 could be significantly down-regulated by CDK7-IN-20 in the cyst-lining epithelial cells of the ADPKD mouse kidney[1].
bPlasma from mouse. PPB was tested at 1 and 10 μM substrate concentrations. bCaco-2 membrane permeability at 10 μM substrate concentrations. The value of 0.133 was determined by quantitative limit (1.0 nM)[1].
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分子量 | 518.57 | |||||||||||||||||||||||||||||||||||||||||||||||
Formula | C30H26N6O3 | |||||||||||||||||||||||||||||||||||||||||||||||
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. |