AMG-900

AMG-900 (AMG900) is a potent, highly selective, orally bioavailable pan-Aurora kinase inhibitor with IC50 of 5, 4 and 1 nM for Aurora A, B and C, respectively; displays excellent specificity in a panel of 26 kinases with exception of p38α and TYK2 (IC50=53 and 220 nM), also exhibits high affinity (Kd< 50 nM) with DDR1, DDR2, and LTK receptor tyrosine kinases; blocks the proliferation of multiple human tumor cell lines including cell lines resistant to paclitaxel, AZD1152, MK-0457, and PHA-739358 with IC50 of 0.7-5.3 nM; blocks the phosphorylation of histone H3 in a dose-dependent manner and significantly inhibits the growth of HCT116 tumor xenografts.Blood Cancer Phase 1 Clinical.