Birinapant
Cat. No.:YN250670
CAS No. :1260251-31-7
产品名称: | Birinapant |
CAS No.: | 1260251-31-7 |
Chemical Name: | (2S,2'S)-N,N'-[(6,6'-difluoro[2,2'-bi-1H-indole]-3,3'-diyl)bis[methylene[(2R,4S)-4-hydroxy-2,1-pyrrolidinediyl][(1S)-1-ethyl-2-oxo-2,1-ethanediyl]]]bis[2-(methylamino)]-propanamide |
Synonyms: | 比瑞那帕; TL32711 |
分子量: | 806.94 |
分子式: | C₄₂H₅₆F₂N₈O₆ |
SMILES: | FC1=CC2=C(C=C1)C(C[C@H]3N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C3)=C(C(N4)=C(C[C@H]5N(C([C@@H](NC([C@@H](NC)C)=O)CC)=O)C[C@@H](O)C5)C6=C4C=C(F)C=C6)N2 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Birinapant (TL32711) 是一种二价 Smac 模拟物,是XIAP和cIAP1的强效拮抗剂,Kd值分别为 45 nM 和小于 1 nM。Birinapant (TL32711) 诱导完整细胞中 cIAP1 和 cIAP2 的自身泛素化和蛋白酶体降解,从而形成 RIPK1: caspase-8 复合物,caspase-8 活化和诱导肿瘤细胞死亡。Birinapant (TL32711) 靶向与 TRAF2 相关的 cIAP,并消除 TNF 诱导的 NF-κB 活化。 |
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Allensworth, J.L., Sauer, S.J., Lyerly, H.K., et al.Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanismBreast Cancer Res. Treat.137(2),359-371(2013)
Krepler, C., Chunduru, S.K., Halloran, M.B., et al.The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cellsClin. Cancer Res.19(7),1784-1794(2013)
Nguyen, Q.D., Lavdas, I., Gubbins, J., et al.Temporal and spatial evolution of therapy-induced tumor apoptosis detected by caspase-3-selective molecular imagingClin. Cancer Res.19(14),3914-3924(2013)