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Entrectinib

Entrectinib

产品编号 T3678   CAS 1108743-60-7
别名: RXDX-101, 恩曲替尼, NMS-E628

Entrectinib (RXDX-101) 是一种可口服的 Trk、ROS1和 ALK 抑制剂,具有抗肿瘤和中枢神经活性,抑制 TrkA、TrkB、TrkC、ROS1 和 ALK 的 IC50值分别为 1、3、5、12 和 7 nM。

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Entrectinib Chemical Structure
Entrectinib, CAS 1108743-60-7
规格 价格/CNY 货期 数量
1 mg ¥ 297 现货
2 mg ¥ 438 现货
5 mg ¥ 722 现货
10 mg ¥ 997 现货
25 mg ¥ 1,670 现货
50 mg ¥ 2,490 现货
100 mg ¥ 3,730 现货
500 mg ¥ 7,530 现货
1 mL * 10 mM (in DMSO) ¥ 889 现货
产品目录号及名称: Entrectinib (T3678)
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纯度: 99.61%
纯度: 99.49%
纯度: 98.03%
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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 Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.
靶点活性 TrkA:1.7 nM, TrkB:0.1 nM, TrkC:0.1 nM, ALK:1.6 nM
体外活性 Entrectinib effectively inhibits ALK‐dependent signaling and specificity blocks proliferation of ALK-dependent cell lines. Entrectinib also significantly inhibits cell growth of the NCI‐H2228 cell line bearing the EML4-ALK rearrangement.
体内活性 In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. [2] In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. [3]
细胞实验 NLF, NLF-TrkB, SY5Y or SY5Y-TrkB cells are plated in 96 well plates, and they are exposed to drug at different concentrations (1, 5, 10, 20, 30, 50 and 100 nM of entrectinib, 1.5 μM Irino and 50 μM TMZ, respectively) for one hr followed by addition of 100 ng/mL of BDNF. Plates are harvested at 24, 48, and 72 hr following addition of drug. The plates are processed and cell viability is analyzed using a standard SRB assay protocol[2].
别名 RXDX-101, 恩曲替尼, NMS-E628
化合物与蛋白结合的复合物

T3678_2

Crystal structure of the ALK kinase domain in complex with Entrectinib

分子量 560.64
分子式 C31H34F2N6O2
CAS No. 1108743-60-7

存储

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

溶解度

Ethanol: 67 mg/mL(119.5 mM)

DMSO: 100 mg/mL (178.36 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 1.7837 mL 8.9184 mL 17.8368 mL 44.5919 mL
5 mM 0.3567 mL 1.7837 mL 3.5674 mL 8.9184 mL
10 mM 0.1784 mL 0.8918 mL 1.7837 mL 4.4592 mL
20 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2296 mL
50 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.8918 mL
100 mM 0.0178 mL 0.0892 mL 0.1784 mL 0.4459 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. Rolfo C, et al. Expert Opin Investig Drugs. 2015, 24(11), 1493-1500. 2. Ardini E, et al. Mol Cancer Ther. 2009, 8, A244. 3. Lyer R, et al. Cancer Res. 2015, 75, 5390.

文献引用

1. Shi S, Ma B, Sun F, et al. Zafirlukast inhibits the growth of lung adenocarcinoma via inhibiting TMEM16A channel activity. Journal of Biological Chemistry. 2022, 298(3). 2. Qin Q, Fu Q, Wang X, et al.Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.European Journal of Medicinal Chemistry.2023: 115291. 3. Jin X, Liu D, Zhou X, et al.Entrectinib inhibits NLRP3 inflammasome and inflammatory diseases by directly targeting NEK7.Cell Reports Medicine.2023, 4(12).
Uniconazole Repotrectinib Taletrectinib Lorlatinib Taletrectinib free base ROS kinases-IN-1 Merestinib ROS kinases-IN-2

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌上市药物库 抗癌药物库 抗癌活性化合物库 酪氨酸激酶分子库 抑制剂库 抗氧化化合物库 经典已知活性库 FDA上市及药典收录分子库 含氟化合物库

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
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% Tween 80
% ddH2O
计算 重置

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

Entrectinib 1108743-60-7 Angiogenesis Autophagy Immunology/Inflammation Tyrosine Kinase/Adaptors Trk receptor ROS ALK ROS Kinase ALK tyrosine kinase receptor Inhibitor Cluster of differentiation 246 RXDX-101 Anaplastic lymphoma kinase (ALK) RXDX 101 RXDX101 恩曲替尼 Trk Receptor inhibit NMS-E628 Tropomyosin related kinase receptor Anaplastic lymphoma kinase CD246 NMS-E-628 NMS-E 628 inhibitor

 

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