TPX-0005 MedChemExpress (MCE)

Product Name	TPX-0005
Synonyms	TPX-0005;Ropotrectinib;1,15-Etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecin-4(5H)-one,11-fluoro-6,7,13,14-tetrahydro-7,13-dimethyl-, (7S,13R)-
CAS	1802220-02-5
EINECS
Chemical Formula	C18H18FN5O2
Molecular Weight	355.3662232
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	Repotrectinib Repotrectinib MedChemExpress (MCE) HY-103022 1802220-02-5 TPX-0005 99.90% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions Repotrectinib Repotrectinib MedChemExpress (MCE) HY-103022 1802220-02-5 TPX-0005 99.90% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. 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. Repotrectinib (TPX-0005) inhibits mutant ALKs including ALK G1202R (IC50=1.26 nM) and ALK L1196M (IC50=1.08 nM). Repotrectinib also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (IC50=1.04, 1.66, 5.3, and 6.96 nM, respectively)[1]. Repotrectinib effectively overcomes this primary resistance (IC50=100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC50=13 nM) and the SRC substrate paxillin (IC50=107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib[1]. Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts[1]. TrkA \| \| \| \| \| \| \| \| \| \| [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. [Content Brief]
Last Update	2025-04-01 14:45:47

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