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Birinapant(TL32711)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Birinapant(TL32711)图片
CAS NO:1260251-31-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)806.94
FormulaC42H56F2N8O6
CAS No.1260251-31-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (123.9 mM)
Water:<1 mg/mL (slightly soluble or insoluble)
Ethanol: 55 mg/mL (68.1 mM)
Solubility (In vivo)15% Captisol: 15mg/mL
SynonymTL32711; TL-32711; TL 32711; SMAC mimetic; Birinapant
Chemical Name(2S,2'S)-N,N'-((2S,2'S)-((3S,3'S,5R,5'R)-5,5'-((6,6'-difluoro-1H,1'H-[2,2'-biindole]-3,3'-diyl)bis(methylene))bis(3-hydroxypyrrolidine-5,1-diyl))bis(1-oxobutane-2,1-diyl))bis(2-(methylamino)propanamide)
实验参考方法
In VitroBirinapant binds with XIAP and cIAP1 with Kd of 45 and<1 nM, respectively. Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells (IC50, ~300 nM), and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells. Birinapant causes rapid cIAP1 degradation, caspase activation, PARP cleavage, and NF-κB activation. Birinapant in combination with TNF-α(1 ng/mL) inhibits the growth of human melanoma cell lines WTH202, WM793B, WM1366 and WM164 with IC50s of 1.8, 2.5, 7.9 and 9 nM, respectively.
In VivoBirinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with.
Animal modelHuman melanoma xenografts 451Lu
Formulation & Dosage12.5% Captisol in distilled water; 30 mg/kg; i.p. 3 times per week
References[1] Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794.
生物活性



Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794.

Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794.