CX-6258 hydrochloride hydrate

Description: CX-6258 HCl hydrate is a novel, potent, selective and orally bioactive pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively. At CX-6258 showed robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. In mechanistic cellular assays with MV-4-11 human AML cells, caused dose-dependent inhibition of the phosphorylation of 2 pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.

References: ACS Med. Chem. Lett., 2012, 3 (2), pp 135–139.

Related CAS #: 1353859-00-3 (HCl salt); 1202916-90-2 (free base); 1353858-99-7 (hydrochloride hydrate)