ASTX660 is an inhibitor of apoptosis proteins found to target BIR3 domain of cIAP1/2 and XIAP through a TNFalpha dependent mechanism in melanoma, breast cancer, and lymphoma cell studies. In a breast cancer xenograft model ASTX660 inhibited tumor growth while displaying no significant adverse effects. Treatment of...

ASTX660 is an inhibitor of inhibitor of apoptosis (IAP) protein-peptide interactions. It inhibits the protein-peptide interaction between the IAP1 and XIAP BIR3 domains with a Smac-derived peptide in cell-free assays (IC50s = 50 = 2.8 nM) and induces displacement of Smac from XIAP in A375 melanoma cells. It induces...