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CDK7-IN-20

CAS No. :

MCE 站：CDK7-IN-20

产品活性：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。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  PI3K/Akt/mTOR

作用靶点：CDK  |  GSK-3

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.

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.
ADME Profiles of CDK7-IN-20 (Compound B2)^a.

	CDK7-IN-20 (Compound B2)
parameters	i.v. 5 mg/kg	s.c. 5 mg/kg
AUClast (hng/mL)	26,937	17,280
AUCIFN_obs (hng/mL)	31,698	17,411
t1/2 (h)	17.8	3.4
Tmax (h)		0.5
Cmax (h)		3806
Cl_obs (mL/min/kg)	2.80
Vss_obs (mL/kg)	1275
MRTIFN_obs (h)	10.2	4.8
F (%)		64.2
plasma protein binding (bound%)b	>99
permeability of Caco-2 A to B Papp (106 cm/s)/B to A Papp (106 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).

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