Description

• AMG 900 is a potent pan-Aurora kinase inhibitor (IC50 values are 1 nM, 4 nM, and 5 nM for Aurora C, B, and A, respectively)
• It is more than 10-fold selective for Aurora kinases over JNK2, Tie2, p38α, Met, and TYK2
• AMG 900 inhibits autophosphorylation of Aurora A and B, as well as the phosphorylation of histone H3 on Ser in HeLa cells
• AMG 900 inhibits proliferation of 26 tumor cell lines (EC50 ranges from 0.7 nM - 5.3 nM), including Paclitaxel (Cat
• No
• 1097)-resistant tumor cell lines
• In an HCT116 tumor xenograft model, AMG 900 inhibits phosphorylation of histone H3 and tumor growth
• It is orally bioavailable.