LY2857785

Research use only, not for human use.

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).

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.

LY 2857785;LY-2857785

Angiogenesis

CDK

CDK

Cancer

——

1619903-54-6

448.60

C26H36N6O

>98% (HPLC)

10 mM in DMSO

CN1C(C(C)C)=C(C(C=C2)=N1)C=C2C3=NC(N[C@H]4CC[C@H](NC5CCOCC5)CC4)=NC=C3

1,4-Cyclohexanediamine, N1-[4-[2-methyl-3-(1-methylethyl)-2H-indazol-5-yl]-2-pyrimidinyl]-N4-(tetrahydro-2H-pyran-4-yl)-, trans-

(-20℃)

With Ice Pack

≥ 2 years