Lisaftoclax (APG-2575) is a novel BCL-2 selective inhibitor with binding Ki of < 0.1/0.1 nM for Bcl-2/Bcl-XL, no binding affinity against BCL-W/MCL-1.
APG-2575 effectively suppressed DLBCL with BCL-2 high expression via activating the mitochondrial apoptosis pathway.
APG-2575 showed strong synergic effect with mouse double minute 2 (MDM2)–p53 inhibitor APG-115 that can achieve potent antitumor effect and markedly prolong survival in animal models.
