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编 号：F756073
分子式：C22H22N4O4S
分子量：438.5
分子式：C22H22N4O4S
分子量：438.5
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CAS No: 2803837-13-8
产品详情
生物活性：
CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research. CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
CDK2/4/6-IN-1(example 29) (25 mg/kg or 50 mg/kg, once a day, orally) has a significant inhibitory effect on tumor growth.The pharmacokinetic parameters of example 29 in BALB/c mice (10 mg/kg, p.o.) ParametersCmax(ng/mL)Tmax(hr)AUClast(hr*ng/mL)T1/2(hr)PO40500.5100504.8The pharmacokinetic parameters of example 29 in BALB/c mice (3 mg/kg, i.v.) ParametersC0(ng/mL)T1/2(hr)AUClast(hr*ng/mL)Vss(L/Kg)IV44070.732450.9
体外研究：
CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits the proliferation of OVCAR3 and MCF7 cells with the IC50 values of 14.6 and 117.8 nM, respectively. CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits phosphorylation of Rb protein in OVCAR3 and MCF7 cells with the IC50 values of 18 and 581 nM, respectively.
CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research. CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
CDK2/4/6-IN-1(example 29) (25 mg/kg or 50 mg/kg, once a day, orally) has a significant inhibitory effect on tumor growth.The pharmacokinetic parameters of example 29 in BALB/c mice (10 mg/kg, p.o.) ParametersCmax(ng/mL)Tmax(hr)AUClast(hr*ng/mL)T1/2(hr)PO40500.5100504.8The pharmacokinetic parameters of example 29 in BALB/c mice (3 mg/kg, i.v.) ParametersC0(ng/mL)T1/2(hr)AUClast(hr*ng/mL)Vss(L/Kg)IV44070.732450.9
体外研究：
CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits the proliferation of OVCAR3 and MCF7 cells with the IC50 values of 14.6 and 117.8 nM, respectively. CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits phosphorylation of Rb protein in OVCAR3 and MCF7 cells with the IC50 values of 18 and 581 nM, respectively.
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