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LY2857785

Chemical Structure : LY2857785

CAS No.: 1619903-54-6

LY2857785 (LY 2857785;LY-2857785)

Catalog No.: PC-42956Not For Human Use, Lab Use Only.

LY2857785 is a potenrt, reversible and ATP-competitive CDK9 inhibitor with IC50 of 11 nM, also inhibits CDK8 (IC50=16 nM) and weakly inhibits CDK7 (IC50=246 nM).

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Biological Activity

LY2857785 is a potenrt, reversible and ATP-competitive CDK9 inhibitor with IC50 of 11 nM, also inhibits CDK8 (IC50=16 nM) and weakly inhibits CDK7 (IC50=246 nM).
LY2857785 showes good selectivity against a panel of 114 protein kinases.
LY2857785 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).
LY2857785 inhibits RNAP II CTD P-Ser2 in vivo, demonstrates potent antitumor growth efficacy in tumor xenografts.

Physicochemical Properties

M.Wt 448.6036
Formula C26H36N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Yin T, et al. Mol Cancer Ther. 2014 Jun;13(6):1442-56.

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