| 应用 |
A selective inhibitor of Bcl-2 |
| 产品介绍 |
ABT-737是 Bcl-xL, Bcl-2 和 Bcl-w抑制剂，EC50分别为78.7 nM，30.3 nM和197.8 nM。对Mcl-1， Bcl-B 和 Bfl-1无抑制性。 |
| 备注 |
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. Phase 2. |
| 生化机理 |
ABT-737 is a pan-Bcl-2 inhibitor that has a wide range of single-agent activity against acute lymphoblastic leukemia (ALL) cell lines and xenografts. Increased expression of the Bcl-2 family of proteins in cancers has been associated with chemotherapy resistance, inhibiting Bcl-2 or Bcl-XL overexpression could potentially induce apoptosis in cancer cells while having minimal effects on normal cells. |
| 别名 |
ABT737;ABT 737; 4-(4-((4'-氯(1,1'-联苯)-2-基)甲基)-1-哌嗪基)-N-((4-(((1R)-3-(二甲基氨基)-1-((苯硫基)甲基)丙基)氨基)-3-硝基苯基)磺酰基)苯甲酰胺;;ABT737;ABT 737;4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4- (dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl] sulfonylbenzamide |
