Repotrectinib(TPX-0005)洛普替尼 ALK/ROS1/TRK抑制剂|CAS 1802220-02-5（53698ES）

Repotrectinib (TPX-0005, TPX0005)，又称洛普替尼，是ALK/ROS1/TRK的抑制剂，作用于ALK、ROS1和TRKA/B/C的IC₅₀为1.01 nM、0.07 nM、0.83 nM、0.05 nM、0.1 nM，具有抗癌活性。Repotrectinib还能抑制突变型ALKs，如ALK (G1202R)和ALK (L1196M)。

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.Karachaliou N, et al. Common Co-activation of AXL and CDCP1 in EGFR-mutation-positive Non-smallcell Lung Cancer Associated With Poor Prognosis. EBioMedicine. 2018 Mar;29:112-127.

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