Cayman LY2857785

LY2857785 is an inhibitor of cyclin-dependent kinase 9 (Cdk9; IC₅₀ = 0.011 µM).¹ It also inhibits Cdk8 and Cdk7 (IC₅₀s = 0.016 and 0.246 µM, respectively), as well as five kinases in a panel of 114 kinases (IC₅₀s = <0.1 µM for all). LY2857785 inhibits proliferation in a panel of 48 patient-derived solid tumor cell lines, including colon, non-small cell lung, and prostate cancer cells, as well as a panel of 24 hematologic tumor cell lines, including acute lymphoblastic leukemia and multiple myeloma cells, with mean IC₅₀ values of 0.22 and 0.197 µM, respectively. It inhibits phosphorylation of DNA-dependent RNA polymerase II (RNAP II) in peripheral blood mononuclear cells (PBMCs) isolated from patients with acute myeloid leukemia (AML) or chronic lymphocytic leukemia (CLL; IC₅₀s = 0.044 and 0.145 µM, respectively). LY2857785 (3, 6, and 9 mg/kg) reduces tumor growth in an MV4-11 rat xenograft model.

WARNING This product is not for human or veterinary use.