| Cas No.: | 1619903-54-6 |
| Chemical Name: | 1,4-Cyclohexanediamine, N1-[4-[2-methyl-3-(1-methylethyl)-2H-indazol-5-yl]-2-pyrimidinyl]-N4-(tetrahydro-2H-pyran-4-yl)-, trans- |
| Synonyms: | LY 2857785;LY-2857785 |
| SMILES: | CC(C)C1N(C)N=C2C=1C=C(C=C2)C1C=CN=C(NC2CCC(NC3CCOCC3)CC2)N=1 |
| Formula: | C26H36N6O |
| M.Wt: | 448.6036 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | LY2857785 is a potenrt, reversible and ATP-competitive CDK9 inhibitor with IC50 of 11 nM, also inhibits CDK8 (IC50=16 nM) and weakly inhibits CSK7 (IC50=246 nM); showes good selectivity against a panel of 114 protein kinases; inhibits RNAP II C-terminal domain (CTD) P-Ser2 and CTD P-Ser5 in U2OS cells with IC50 of 89 and 42 nM, dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines (MV-4-11 cell IC50=40 nM); inhibits RNAP II CTD P-Ser2 in vivo, demonstrates potent antitumor growth efficacy in tumor xenografts. |

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