Chemical Name:A-1155463 Hydrochloride
Application Notes:A-1155463 Hydrochloride, is a potent and selective BCL-XL inhibitor with in vivo activity. A-1155463 is a proteolytically stable, cell-permeable and high affinity BH3 mimetic Ligand of BCL protein BCL-XL, binding to the target potently and selectively with a Ki value of<0.01nM (<10 highly="" selective="" against="" closely="" related="" proteins="" of="" bcl-2="" ki="74nM,">7000-fold selectivity), BCL-W (Ki = 8 nM, >800-fold selectivity), and MCL-1 (Ki >444nM, >40000-fold selectivity). A-1155463, together with A-1331852 , represent the first-in-class small molecule BCL-XL selective inhibitors achieving clear-on-target in vivo activity with high potency and selectivity. In living cells, A-1155463, as anticipated, experts an effort to disrupt the tight-binding BCL-XL-BIM, but not BCL-2–BIM, complexes, killing BCL-XL–dependent Molt-4 cells (EC50=70nM) without measurable cytotoxicity against BCL-2–dependent RS4 (ref. 1), inducing the hallmarks of intrinsic apoptosis (ref. 1).
Melting Pt.:>140°C (dec.)
Boiling Pt.:No Data Available
Solubility:No Data Available
Storage Condition:-20°C Freezer, Under inert atmosphere