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编 号：F762890
分子式：C30H26N6O3
分子量：518.57
分子式：C30H26N6O3
分子量：518.57
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CAS No: 3034210-97-1
产品详情
生物活性：
CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC50 value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.
体内研究：
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)
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 ratioc48.0
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).Animal Model:Neonatal Pkd1flox/flox:Ksp-Cre mice
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.
体外研究：
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.
CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC50 value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research.
体内研究：
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)
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 ratioc48.0
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).Animal Model:Neonatal Pkd1flox/flox:Ksp-Cre mice
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.
体外研究：
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.
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