CDK2/4/6-IN-1

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[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

CDK2:2.5 nM (IC50)

CDK4:23.7 nM (IC50)

CDK6:44.3 nM (IC50)

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[1]. 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[1].

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[1]. The pharmacokinetic parameters of example 29 in BALB/c mice (10 mg/kg, p.o.) Parameters Cmax(ng/mL) Tmax(hr) AUClast(hr*ng/mL) T1/2(hr) PO 4050 0.5 10050 4.8The pharmacokinetic parameters of example 29 in BALB/c mice (3 mg/kg, i.v.) Parameters C0(ng/mL) T1/2(hr) AUClast(hr*ng/mL) Vss(L/Kg) IV 4407 0.7 3245 0.9

[1]. ZHANG YAN, et al. Cdk2/4/6 inhibitor, preparation method therefor, and application thereof. WO2022152259 A1.