Chemical Name: 4-[4-[[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
Biological ActivitySelective, high affinity Bcl-2 inhibitor (Ki < 0.010 nM). Exhibits >4800-fold selectivity for Bcl-2 over Bcl-xL and Bcl-w, and displays no measurable activity at Mcl-1 (Ki > 444 nM). Potently induces apoptosis in FL5.12-BCL-2 cells (EC50 = 261 nM) and reduces tumor burden in chronic lymphocytic leukemia (CLL) primary samples (EC50 = 3 nM). Shows reduced toxicity to platelets compared to similar compounds. Enhances efficacy of clinically relevant chemotherapy and immunotherapy drugs. Orally bioavailable. Exhibits binding to SARS-CoV-2 3C-like protease (3CLpro) active site in a virtual screen.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
Souers et al.
Systematic mapping of BCL-2 gene dependencies in cancer reveals molecular determinants of BH3 mimetic sensitivity.
Soderquist et al.
Balancing apoptosis and autophagy for Parkinson's disease therapy: targeting BCL-2.
Liu et al.
ACS Chem.Neurosci., 2019;10:792
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