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  5. Tocris Bioscience™ ABT 199

Tocris Bioscience™ ABT 199
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Product Code. 18778046
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Product Code. 18778046 Supplier Tocris Bioscience™ Supplier No. 6960/50

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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.
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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 50 mg
Target Bcl-2 Family Inhibitors
Molecular Formula C45H50ClN7O7S
Formula Weight 868.45
Product Type Inhibitor
Purity 98%
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