| 应用 |
A Bcl-2-selective inhibitor with Ki of <0.01 nM |
| 产品介绍 |
ABT-199 (GDC-0199)是高效的Bcl-2选择性抑制剂，Ki为0.01 nM，比对Bcl-xL和Bcl-w的抑制性高4800倍以上，对Mcl-1无活性。 |
| 备注 |
ABT-199 (GDC-0199) is a Bcl-2-selective inhibitor with Ki of <0.01 nM, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Phase 2. |
| 生化机理 |
ABT-199 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, currently in clinical trials. ABT-199 inhibits the growth of BCL-2-dependent tumors in vivo and spares human platelets. A single dose of ABT-199 in three patients with refractory chronic lymphocytic leukemia resulted in tumor lysis within 24 h. These data indicate that selective pharmacological inhibition of BCL-2 shows promise for the treatment of BCL-2-dependent hematological cancers. |
| 别名 |
GDC-0199;GDC-0199;ABT199;ABT 199;GDC0199;GDC 0199;Venetoclax ; abt 199;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 |
