A-1331852 (A1331852) is a potent and selective BCL-XL inhibitor (Ki<10 pM).
A-1331852 shows much weaker affinity for BCL-2 (Ki=6 nM), BCL-W (Ki=4 nM), and MCL-1 (Ki=142 nM).
A-1331852 selectively disrupts BCL-XL–BIM complexes and induces the hallmarks of apoptosis in BCL-XL–dependent Molt-4 cells (Molt-4 viability IC50=6 nM).
A-1331852 demonstrates antitumor efficacy in the Molt-4 xenograft model; orally active.
