Birinapant|1260251-31-7|(比瑞那帕; TL32711)-陌孚医药/Medlife

您当前的位置：

Birinapant (Synonyms: 比瑞那帕; TL32711)

目录号: PL04631 纯度: ≥99%

CAS No. :1260251-31-7

商品编号	规格	价格	会员价
PL04631-2mg	2mg	¥1050.91	请登录
PL04631-5mg	5mg	¥1730.91	请登录
PL04631-10mg	10mg	¥2720.00	请登录
PL04631-50mg	50mg	¥8036.36	请登录
PL04631-100mg	100mg	¥12301.82	请登录
PL04631-200mg	200mg	询价	询价
PL04631-500mg	500mg	询价	询价
PL04631-10mM*1mLinDMSO	10mM*1mLinDMSO	¥2414.62	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称	Birinapant
中文别名	Birinapant 抑制剂;比瑞那帕;Birinapant
英文名称	Birinapant
英文别名	(2S)-N-[(2S)-1-[(2R,4S)-2-[[6-fluoro-2-[6-fluoro-3-[[(2R,4S)-4-hydroxy-1-[(2S)-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]pyrrolidin-2-yl]methyl]-1H-indol-2-yl]-1H-indol-3-yl]methyl]-4-hydroxypy;Birinapant;TL32711;TL-32711;(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;Birinapant (TL32711);TL 32711;6O4Z07B57R;(2S)-N-[(2S)-1-[(2R,4S)-2-[[6-fluoro-2-[6-fluoro-3-[[(2R,4S)-4-hydroxy-1-[(2S)-2-[[(2S)-2-(methylamino)propanoyl]amino]butanoyl]pyrrolidin-2-yl]methyl]-1H-indol-2-yl]-1H-indol-3-yl]methyl]-4-hydroxypyrrolidin-1-yl]-1-oxobutan-2-yl]-2-(methylamino)propanamide;(2s,2's)-N,N'-[(6,6'-Difluoro-1h,1'h-2,2'-Biindole-3,3'-Diyl)bis{methanediyl[(2r,4s)-4-Hydroxypyrrolidine-2,1-Diyl][(2s)-1-Oxobutane-1,2-Diyl]}
Cas No.	1260251-31-7
分子式	C₄₂H₅₆F₂N₈O₆
分子量	806.94
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Birinapant (TL32711) 是一种二价 Smac 模拟物，是 XIAP 和 cIAP1 的强效拮抗剂，K_d 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

生物活性

Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with K d s of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation.

性状

Solid

IC50 & Target[1][2]

Kd: 45 nM (XIAP), <1 nM (cIAP1)

体外研究(In Vitro)

Birinapant (TL32711) (30-10000 nM; 24 hours) significantly decreases the viability of SUM190 cells in a dose-dependent manner.
Birinapant (TL32711) (30-1000 nM; 4 hours) shows a significant decrease in cIAP1 levels and enhanced PARP cleavage, and induces apoptosis.
Birinapant (TL32711) binds with high affinity to the isolated BIR3 domains of cIAP1, cIAP2, and XIAP and the single BIR domain of ML-IAP and rapidly degrades TRAF2-bound cIAP1 and cIAP2 thereby inhibiting TNF-mediated NF-κB activation. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Birinapant (TL32711) (30 mg/kg; i.p.; every third day (*5)) shows antitumor efficacy and are devoid of overt toxicity in preclinical models. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Allensworth JL, et al. Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism. Breast Cancer Res Treat. 2013 Jan;137(2):359-71.
[2]. Krepler C, et al. The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. Clin Cancer Res. 2013 Apr 1;19(7):1784-94.

溶解度数据	In Vitro: DMSO : 125 mg/mL (154.91 mM; Need ultrasonic)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation