CDK7-IN-20

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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。

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)
parameters	i.v. 5 mg/kg	s.c. 5 mg/kg
AUC_last(h·ng/mL)	26,937	17,280
AUC_{IFN_obs}(h·ng/mL)	31,698	17,411
t_1/2(h)	17.8	3.4
T_max(h)		0.5
C_max(h)		3806
Cl_{_obs}(mL/min/kg)	2.80
V_{ss_obs}(mL/kg)	1275
MRT_{IFN_obs}(h)	10.2	4.8
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 ratio^c	<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 Pkd1^flox/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.