Description
InformationCDKI-73 (LS-007) is a potentCDKinhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficaciousCDK9inhibitor against acute myeloid leukemia.TargetsCDK2 (Cell-free assay); CDK9 (Cell-free assay); CDK1 (Cell-free assay); CDK4 (Cell-free assay) 3.27 nM; 5.78 nM; 8.17 nM; 8.18 nMIn vitroCDKI-73 induces cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9. Contrastively, it is relatively low toxic to the bone marrow cells of healthy donors.In vivoCDKI-73 is orally bioavailable, highly efficacious against MLL-AML MV4–11 xenografts and downregulates anti-apoptotic proteins by targeting CDK9 in vivo.Cell Research(from reference)Cell lines：Leukemia cell lines (MOLM13, MV4-11, THP-1, etc.) Concentrations：0.05 µM, 0.1 µM, 0.25 µM, 0.5 µM Incubation Time：1 h, 4 h, 12 h, 24 h, 48 h