Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound acting as a reversible and ATP-competitive inhibitor of Cdk4/6 (IC50 = 1.5 µM and 5.6 µM for Cdk4/D1 and Cdk6/D1, respectively) with selectivity over Cdk5/p35 (IC50 = 25 µM), v-abl, c-met, IGF-1R and IR (IC50 > 10 µM), Cdk2/A, Cdk2/E, Cdk4/D2, Cdk6/D2 (IC50 > 50 µM) and Cdk1/B (IC50 > 100 µM). Cdk4/6 Inhibitor IV exhibits blocking of pRb phosphorylation at Ser780 and Ser795, induce cell cycle arrest (G0/G1), and apoptosis in U2OS and MRC-5 cells at 5 - 10 µM. Further, suppresses tumor growth in Xenograft mouse model (30 mg/kg, i.p.).
Soni, R., et al. 2001. J. Natl. Cancer Inst. 93, 436.
See how others have used Cdk4/6 Inhibitor IV. Click on the entry to view the PubMed entry .
PMID: # 26851223 2016. J. Immunol. 196: 2870-8.
PMID: # 27192561 2016. Cell Cycle. 15: 1787-95.
PMID: # 11259469 Soni, R. et al. 2001. J. Natl. Cancer Inst. 93: 436-446.
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