S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor, with Kis and Kds of 1.3 nM, 520 nM and 3.9 nM, 186 nM for BCL-2 and BCL-XL, respectively. S55746 hydrochloride has antitumor activity.
S55746 hydrochloride is a potent, orally active and selective BCL-2 inhibitor, with Kis and Kds of 1.3 nM, 520 nM and 3.9 nM, 186 nM for BCL-2 and BCL-XL, respectively. S55746 selectively induces cell death. S55746 potently causes RS4;11 cell killing with an IC50 of 71.6 nM after 72 h of treatment, but shows a much weaker activity in H146 (IC50 1.7 μM), a BCL-XL-dependent cell line. S55746 also selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner. S55746 (3 nM) induces cell death in CLL cells[1].
S55746 is a highly efficacious and well-tolerated orally active BCL-2 inhibitor. S55746 (25 and 100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models[1].
[1]. Casara P, et al. S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth. Oncotarget. 2018 Apr 13;9(28):20075-20088.