SGI-1776

SGI-1776 is a potent, selective, orally active Pim kinase inhibitor with IC50 of 7, 363 and 69 nM for Pim1, Pim2 and Pim3, respectively; exhibits promising selectivity against a panel of >300 kinases, shows inhibitory activity against two other kinases: Flt-3 (IC50=44 nM) and Haspin (IC50=34 nM) ; reduces cell viability of androgen-independent prostate cancer cell lines with IC50 of 2-4 uM, causes cell cycle arrest and caspase-dependent apoptosis in prostate cancer cells, marginally sensitizes prostate cancer cells to taxane-based therapeutics by inhibiting MDR1 activity and inducing apoptosis; shows efficacy in xenograft model bearing MV-4-11 tumors.Prostate Cancer Phase 1 Clinical.