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Entrectinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Entrectinib图片
CAS NO:1108743-60-7
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
RXDX-101
NMS-E628
恩曲替尼
产品介绍
Entrectinib 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。

产品描述

Entrectinib 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.

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].

Cas No.

1108743-60-7

分子式

C31H34F2N6O2

分子量

560.65

别名

RXDX-101;NMS-E628;恩曲替尼

储存和溶解度

Ethanol:67 mg/mL(119.5 mM)
DMSO:100 mg/mL (178.36 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years