Repotrectinib

Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM) . Repotrectinib has anti-cancer activity[1][2].

Product Specifications

CAS Number

[1802220-02-5]

Product Name Alternative

TPX-0005

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Anaplastic lymphoma kinase (ALK) ; ROS Kinase; Trk Receptor

Type

Reference compound

Related Pathways

Neuronal Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TPX-0005.html

Purity

99.93

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C1NC[C@H](C)OC2=CC=C(F)C=C2[C@@H](C)NC3=NC4=C1C=NN4C=C3

Molecular Formula

C18H18FN5O2

Molecular Weight

355.37

Precautions

H302, H315, H319, H335

References & Citations

[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.