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CDK7-IN-20
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CDK7-IN-20图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CDK7-IN-20 是一种有效的、选择性的、不可逆的CDK7(CDK) 抑制剂,IC50值为 4 nM。CDK7-IN-20 对 CDK7 的选择性超过 CDK1、CDK2、CDK3、CDK5、CDK6、CDK9 和 CDK12 的 206 倍以上。CDK7-IN-20 具有用于常染色体显性多囊肾病 (ADPKD) 研究的潜力。
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]

CDK7

4 nM (IC50)

CDK1

3375 nM (IC50)

CDK2

823 nM (IC50)

CDK3

1837 nM (IC50)

CDK5

>10,000 nM (IC50)

CDK6

950 nM (IC50)

CDK9

526 nM (IC50)

CDK12

>10,000 nM (IC50)

GSK3β

148 nM (IC50)

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].
ADME Profiles of CDK7-IN-20 (Compound B2)a[1].

CDK7-IN-20 (Compound B2)
parametersi.v. 5 mg/kgs.c. 5 mg/kg
AUClast(h·ng/mL)26,93717,280
AUCIFN_obs(h·ng/mL)31,69817,411
t1/2(h)17.83.4
Tmax(h)0.5
Cmax(h)3806
Cl_obs(mL/min/kg)2.80
Vss_obs(mL/kg)1275
MRTIFN_obs(h)10.24.8
F (%)64.2
plasma protein binding (bound%)b>99
permeability of Caco-2 A to B Papp (10–6 cm/s)/B to A Papp (10–6 cm/s)/efflux ratioc<0.133/6.370/>48.0
aThree ICR mice were used for each group. The data are expressed as mean values.
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].

Animal Model:Neonatal Pkd1flox/flox:Ksp-Cre mice[1]
Dosage:5 mg/kg
Administration:Subcutaneous administration; once daily; for 6 days
Result:Significantly reduced the kidney size and cyst formation of the ADPKD mice.
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.