CDK4/6-IN-7

CDK4/6-IN-7 is a potent, selective and orally active CDK4/6 inhibitor, with IC50s of 1.58 and 4.09 nM, respectively. CDK4/6-IN-7 can be used for the research of breast cancer[1].

Research Areas >> Cancer

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

CDK4:1.58 nM (IC50)

CDK6:4.09 nM (IC50)

CDK4/6-IN-7 (compound 7c) (0.1-656.1 µM; 48 h) inhibits the viability of MCF-7 cells, with an IC50 of 0.92 μM[1]. Cell Proliferation Assay[1] Cell Line: MCF-7 cells Concentration: 0.1, 0.3, 0.9, 2.7, 8.1, 24.3, 72.9, 218.7, 656.1 µM Incubation Time: 48 hours Result: Inhibited MCF-7 cells growth, with an IC50 of 0.92 μM.

CDK4/6-IN-7 (compound 7c) (50 mg/kg; p.o. once daily for 7d) strongly reduces tumor growth rates in MCF-7 tumor-bearing mice[1]. Animal Model: Female nude mice (5 weeks) bearing MCF-7 tumor[1] Dosage: 50 mg/kg Administration: Oral gavage once daily for 7 days Result: Inhibited tumor growth with the tumor inhibition rate of 57.68% and was well tolerated.

[1]. Liang JW, et, al. Synthesis and identification of a novel skeleton of N-(pyridin-3-yl) proline as a selective CDK4/6 inhibitor with anti-breast cancer activities. Bioorg Chem. 2022 Feb;119:105547.