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Birinapant

Birinapant

产品编号 T6007   CAS 1260251-31-7
别名: TL32711, 比瑞那帕

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。它靶向与 TRAF2 相关的 cIAP,并消除 TNF 诱导的 NF-κB 活化。

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Birinapant Chemical Structure
Birinapant, CAS 1260251-31-7
规格 价格/CNY 货期 数量
1 mg ¥ 459 现货
2 mg ¥ 666 现货
5 mg ¥ 1,110 现货
10 mg ¥ 1,770 现货
25 mg ¥ 2,860 现货
50 mg ¥ 3,720 现货
100 mg ¥ 5,330 现货
1 mL * 10 mM (in DMSO) ¥ 1,620 现货
产品目录号及名称: Birinapant (T6007)
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纯度: 99.59%
纯度: 99.47%
纯度: 98.32%
纯度: 98%
纯度: 97.42%
纯度: 97.08%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.
靶点活性 XIAP:45 nM(Kd), cIAP1:<1 nM(Kd)
体外活性 Birinapant 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. [1] Birinapant in combination with TNF-α exhibits a strong antimelanoma effect in vitro. 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, while neither compound is effective individually. Birinapant singly treatment induces inhibition on proliferation of WM9 cells with IC50 of 2.4 nM. Birinapant significantly inhibits the target protein cIAP1 and cIAP2 in these cell lines.[2]
体内活性 Birinapant (30 mg/kg) treatment significantly induces abrogation of tumor growth in melanoma xenotransplantation models 451Lu with. [2]
激酶实验 Fluorescence polarization assay: The binding affinities of compounds to XIAP and cIAP1 are determined using a fluorogenic substrate and are reported as Kd values. Initially, the dissociation constant (Kd) for the fluorescently labeled modified Smac peptide (AbuRPF-K(5-Fam)-NH2; FP pep-tide) is determined using a fixed concentration of peptide (5 nM) and titrating varying concentrations of protein (0.075–5 μM in half log dilutions). The dose–response curves are produced by a nonlinear least squares fit to a single-site binding model using GraphPad Prism, with 5 nM of FP peptide and 50 nM of XIAP used in the assay. Various concentrations of Smac mimetics (100–0.001 μM in half log dilutions) are added to FP peptide:protein binary complex for 15 min at room temperature in 100μL of 0.1 M potassium phosphate buffer, pH 7.5, containing 100 mg/mL bovine c -globulin. Following incubation, the polarization values are measured on a multi-label plate reader using a 485 nm excitation filter and a 520 nm emission filter.
细胞实验 Cells are allowed to attach for 24 hours and subsequently incubated with Birinapant and/or TNF-α for 24 or 72 hours. Then MTS assay is conducted(Only for Reference)
别名 TL32711, 比瑞那帕
分子量 806.94
分子式 C42H56F2N8O6
CAS No. 1260251-31-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 51 mg/mL (63.2 mM)

DMSO: 93 mg/mL (115.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 1.2392 mL 6.1962 mL 12.3925 mL 30.9812 mL
5 mM 0.2478 mL 1.2392 mL 2.4785 mL 6.1962 mL
10 mM 0.1239 mL 0.6196 mL 1.2392 mL 3.0981 mL
20 mM 0.062 mL 0.3098 mL 0.6196 mL 1.5491 mL
50 mM 0.0248 mL 0.1239 mL 0.2478 mL 0.6196 mL
DMSO 100 mM 0.0124 mL 0.062 mL 0.1239 mL 0.3098 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Allensworth JL, et al. Breast Cancer Res Treat, 2013, 137(2), 359-371. 2. Krepler C, et al. Clin Cancer Res, 2013, 19(7), 1784-1794. 3. Bhatt S, Pioso M S, Olesinski E A, et al. Reduced Mitochondrial Apoptotic Priming Drives Resistance to BH3 Mimetics in Acute Myeloid Leukemia[J]. Cancer Cell,. 2020

文献引用

1. Bhatt S, Pioso M S, Olesinski E A, et al. Reduced Mitochondrial Apoptotic Priming Drives Resistance to BH3 Mimetics in Acute Myeloid Leukemia. Cancer Cell. 2020, 38(6): 872-890. e6.
Momordin Ic NVP-HSP990 Alda-1 JHU395 Actein Pantoprazole sodium 14-Deoxyandrographolide Ziyuglycoside II

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌活性化合物库 抗癌临床化合物库 经典已知活性库 药物功能重定位化合物库 铜死亡化合物库 抗肺癌化合物库 ReFRAME 相关化合物库 抗感染化合物库 抗病毒库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Birinapant 1260251-31-7 Apoptosis Microbiology/Virology Proteases/Proteasome IAP HIV Protease inhibit Inhibitor TL-32711 HIV Human immunodeficiency virus TL 32711 TL32711 比瑞那帕 inhibitor

 

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