Information CDKI-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. Targets CDK2 (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 nM In vitro CDKI-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 vivo CDKI-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
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CDKI-73
CAS number:1421693-22-2 molecular formula:C15H15FN6O2S2
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| Chinese alias | - | ||
| English alias | GAIOPWBQKZMUNO-UHFFFAOYSA-N | MS-26626 | 3-((5-fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl)pyrimidin-2-yl)amino)benzenesulfonamide | A925431 | GTPL12074 | 3,4-Dihydroxyphenylserine | AKOS030526509 | (+-)-1-(2-Piperidinyl)-2-propanone | 3-({5-fluoro-4-[ | ||
| CAS number | 1421693-22-2 | molecular formula | C15H15FN6O2S2 |
| molecular weight | 394.45 g/mol | Exact mass | - |
| PSA | 160.000 Ų | logp | 2.359 |
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