High affinity XIAP antagonist; active in vivo
| Cas No. | 762274-58-8 |
| 别名 | N-甲基-L-丙氨酰-(2S)-2-环己基氨基乙酰基-N-[(1R)-1,2,3,4-四氢-1-萘基]-L-脯氨酰胺盐酸盐 |
| Canonical SMILES | CN[C@H](C(N[C@H](C(N1CCC[C@H]1C(N[C@@H]2CCCC3=CC=CC=C23)=O)=O)C4CCCCC4)=O)C.Cl |
| 分子式 | C27H40N4O3.HCl |
| 分子量 | 505.09 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | High affinity XIAP antagonist (Kd = 16 nM for the BIR3 domain of XIAP). Exhibits cytotoxicity in a wide range of cancer cell lines in vitro (EC50 = 13 nM in MDA-MB-231 cells). Also displays antitumor activity in a mouse breast cancer xenograft model. Enhances TRAIL-induced apoptosis in chronic lymphocytic leukemia (CLL) cells. Oost et al (2004) Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J.Med.Chem. 47 4417 PMID:15317454 |Loeder et al (2009) A novel paradigm to trigger apoptosis in chronic lymphocytic leukemia. Cancer Res. 69 8977 PMID:19920200 |
