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首页-小分子抑制剂&激动剂-Apoptosis-IAP-Birinapant
Birinapant

Chemical Structure : Birinapant

CAS No.: 1260251-31-7

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Birinapant (TL32711, TL 32711)

货号: PC-21402Not For Human Use, Lab Use Only.

Birinapant (TL32711) is a bivalent, selective small molecule SMAC mimetic, binds with high affinity to multiple members of the IAP family with Kd of 45 nM and <1 nM for XIAP and cIAP1 respectively.

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10 mg ￥1480 In stock
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50 mg ￥4280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Birinapant (TL32711) is a bivalent, selective small molecule SMAC mimetic, binds with high affinity to multiple members of the IAP family with Kd of 45 nM and <1 nM for XIAP and cIAP1 respectively.
Birinapant (TL32711) binds to the BIR3 domains of cIAP1, cIAP2, XIAP, and the BIR domain of ML-IAP in vitro.
v specifically targets cIAP1 and cIAP2 for degradation, resulting in a switch in TNFR signaling; activation of TNFR upon binding of TNF-α in the presence of cIAP1 and cIAP2 leads to NF-κB activation and increased cell proliferation.
Birinapant (TL32711) in combination with TNF-α elicites anti-melanoma effect in a parental and BRAF inhibitor resistant cell line.
Birinapant (TL32711) preferentially targets the TRAF2-associated cIAP1 and cIAP2 with subsequent inhibition of TNF-induced NF-κB activation.
Birinapant (TL32711) inhibits umor growth in multiple primary patient-derived xenotransplant models.

物理化学性质&存储条件

分子量 806.96
分子式 C42H56F2N8O6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(2S,2'S)-N,N'-((2S,2'S)-((3S,3'S,5R,5'R)-((6,6'-difluoro-1H,1'H-[2,2'-biindole]-3,3'-diyl)bis(methylene))bis(3-hydroxypyrrolidine-5,1-diyl))bis(1-oxobutane-1,2-diyl))bis(2-(methylamino)propanamide)

参考文献

1. Benetatos CA, et al. Mol Cancer Ther. 2014 Apr;13(4):867-79.

2. Krepler C, et al. Clin Cancer Res. 2013 Apr 1;19(7):1784-94.

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