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Birinapant

Birinapant

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

Birinapant 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, CAS 1260251-31-7
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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 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 cIAP1:<1 nM(Kd), XIAP:45 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 2 years

溶解度

Ethanol: 51 mg/mL (63.2 mM)

DMSO: 93 mg/mL (115.3 mM)

H2O: <1 mg/mL

( < 1 mg/mL refers to the product slightly soluble or insoluble )

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.
Absinthin Schisantherin D AMD 3465 (S)-BI-1001 Jacoumaric acid Calanolide E Licoarylcoumarin Vitexilactone

相关化合物库

该产品包含在如下化合物库中:
含氟化合物库 抗结直肠癌化合物库 抗卵巢癌化合物库 抗癌化合物库 抗肺癌化合物库 抗癌活性化合物库 铜死亡化合物库 血液病分子库 已知活性化合物库 临床期小分子药物库

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。
% DMSO
%
% Tween 80
% ddH2O
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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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X
X
X
=
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g/mol

输入分子式,点击计算,可计算出产品的分子量。

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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 HIV Protease IAP TL32711 TL-32711 inhibit Inhibitor TL 32711 HIV Human immunodeficiency virus 比瑞那帕 inhibitor

 

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