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
| Marque | Tocris |
|---|---|
| Réf. B-LABO | BL-RE-151385 |
| Réf. fabricant | 18778736 |
| Nom chimique ou matériau | 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 |
| Synonyme | GDC-0199 |
| Quantité | 10 mg |
| Cible | Bcl-2 Family Inhibitors |
| Formule moléculaire | C<sub>45</sub>H<sub>50</sub>ClN<sub>7</sub>O<sub>7</sub>S |
| Poids de la formule | 868.45 |
| Type de produit | Inhibitor |
| Pureté | 98% |
