恩曲替尼 T3678

Product Introduction
Bioactivity


英文名: Entrectinib

描述: 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。

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].

体外活性: Entrectinib有效抑制ALK依赖性信号传导，并特异性阻断ALK依赖性细胞系的增殖。Entrectinib还显著抑制带有EML4-ALK重排的NCI-H2228细胞系的细胞增长。

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]

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

溶解度: Ethanol : 67 mg/mL(119.5 mM)
DMSO : 50 mg/mL (89.18 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
5% DMSO+95% Saline : 5 mg/mL (8.92 mM, suspension)


关键字: ROS Kinase | ALK tyrosine kinase receptor | Inhibitor | Cluster of differentiation 246 | Anaplastic lymphoma kinase (ALK) | Autophagy | RXDX 101 | RXDX101 | Trk Receptor | inhibit | Tropomyosin related kinase receptor | Anaplastic lymphoma kinase | CD246 | NMS-E-628 | Entrectinib | NMS-E 628

相关产品: Crizotinib hydrochloride | ROS kinases-IN-2 | HS-291 | ROS-generating agent 1 | Anti-inflammatory agent 64 | Salvigenin | Taletrectinib free base | Uniconazole | F-1 | Taletrectinib

相关库: FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Tyrosine Kinase Inhibitor Library | EMA Approved Drug Library

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