Tocris Bioscience™ ABT 199

Description

Selective, high affinity Bcl-2 inhibitor; orally bioavailable

ABT 199 is a selective, 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. ABT 199 reverses oxidative phosphorylation in acute myeloid leukemia cells (AML), in vitro and in vivo.

Specifications

• Chemical Name or Material: 4-[4-[[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2 H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1 H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
• CAS: 1257044-40-8
• Synonym: GDC-0199
• Quantity: 10 mg
• Target: Bcl-2 Family Inhibitors
• Molecular Formula: C₄₅H₅₀ClN₇O₇S
• Formula Weight: 868.45
• Product Type: Inhibitor
• Purity: 98%