| 名称 | Entrectinib |
| 描述 | Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1/3/5/12/7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity. |
| 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 | 方法: 人肺癌细胞 HCC78 用 Entrectinib (0.1-10 µM) 处理 72 h，使用 CCK-8 assay 检测细胞活力。
结果: Entrectinib 有效抑制细胞存活，抑制 HCC78 的 IC50 值为 450 nM。[1]
方法: 大肠癌细胞 KM12 用 Entrectinib (10-250 nmol/L) 处理 2 h，使用 Western Blot 检测靶点蛋白表达水平。
结果: Entrectinib 在处理 2 h 后消除了 TPM3-TRKA 的自磷酸化，同时完全抑制了 PLCγ1、AKT 和 MAPK 的磷酸化。[2] |
| 体内活性 | 方法: 为检测体内抗肿瘤活性，将 Entrectinib (30-60 mg/kg) 口服给药给携带 Karpas-299 异种移植物的 SCID 小鼠，每天两次，持续十天。
结果: 两种剂量水平都是有效的，可以诱导所有肿瘤消退到无法触及的程度。在停止 60 mg/kg 剂量的治疗后的观察期内，在治疗结束后第 80 天，7 只小鼠中有 4 只持续根除肿瘤，而在所有接受 30 mg/kg 剂量治疗的动物中都观察到肿瘤再生。[2] |
| 存储条件 | Store at low temperature
Pure form: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : 67 mg/mL (119.51 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (17.84 mM), Solution.
DMSO : 260 mg/mL (463.76 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+90% Saline : < 10 mg/mL (17.84 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+ 5% Tween 80 + 45% Saline : 10 mg/mL (17.84 mM), Solution.
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| 关键字 | Tropomyosin related kinase receptor | Trkreceptor | TrkC | TrkB | TrkA | Trk Receptor | RXDX101 | RXDX 101 | ROSKinase | ROS1 | ROS Kinase | ROS | NMS-E-628 | NMS-E 628 | Inhibitor | inhibit | Entrectinib | Cluster of differentiation 246 | CD246 | Autophagy | Anaplastic lymphoma kinase (ALK) | Anaplastic lymphoma kinase | ALK tyrosine kinase receptor | ALK |
| 相关产品 | Allopurinol | Kaolin | Guanidine hydrochloride | Naringin | Aceglutamide | Alginic acid | Hemin | Hydroxychloroquine | Stavudine | Ethoxyquin | Paeonol | Ethyl linoleate |
| 相关库 | 抗癌上市药物库 | 抗癌活性化合物库 | 临床失败化合物库 | 激酶抑制剂库 | 经典生物活性库 | 抗衰老化合物库 | 生物活性化合物库 | FDA 上市药物库 | 膜蛋白靶向化合物库 | 免疫/炎症分子化合物库 | FDA 上市激酶抑制剂库 | 抗癌药物库 |