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Repotrectinib

Repotrectinib (TPX-0005) 是ROS1(IC50=0.07 nM) 和TRK(对 TRKA/B/C 的IC50=0.83/0.05/0.1 nM) 抑制剂，能够抑制 WTALK(IC50=1.01 nM)。它具有抗癌作用。

CAS号

1802220-02-5

分子式

C18H18FN5O2

主要靶点

ROS|Src|ROS Kinase|ALK|Trk receptor

仅限科研使用

Cat No : CM02613

Print datasheet

Synonyms

TPX-0005|TPX 0005|TPX0005

验证数据展示

  • CAS No.: 1802220-02-5

    Repotrectinib
    CAS#: 1802220-02-5

产品信息

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.

CAS号 1802220-02-5
分子式 C18H18FN5O2
主要靶点 ROS|Src|ROS Kinase|ALK|Trk receptor
主要通路 蛋白酪氨酸激酶|免疫与炎症|血管生成
分子量 355.37
纯度 99.86%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 TPX-0005|TPX 0005|TPX0005

靶点活性

Src:5.3 nM|WT ALK:1.01 nM|ALK(L1196M):1.08 nM|ALK(G1202R):1.26 nM

溶解度

DMSO:83.3 mg/mL

参考文献

1.Dayong Zhai, et al. Abstract 2132: The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors. Cancer Research. July 2016
2.Li W, Perpinioti N, Schinkel A H, et al. Bioanalytical assay for the new-generation ROS1/TRK/ALK inhibitor repotrectinib in mouse plasma and tissue homogenate using liquid chromatography-tandem mass spectrometry[J]. Journal of Chromatography B. 2020: 122098.

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