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Repotrectinib

Names

[ CAS No. ]:
1802220-02-5

[ Name ]:
Repotrectinib

[Synonym ]:
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)-
08O3FQ4UNP
(3R,11S)-6-Fluoro-3,11-dimethyl-10-oxa-2,13,17,18,21-pentaazatetracyclo[13.5.2.04,9.018,22]docosa-1(21),4,6,8,15(22),16,19-heptaen-14-one
Repotrectinib

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ROS
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Trk Receptor
Research Areas >> Cancer

[Target]

IC50: 5.3 nM (SRC), 1.01 nM (WT ALK), 1.26 nM (ALK G1202R), 1.08 nM (ALK L1196M)[1]


[In Vitro]

Repotrectinib (TPX-0005) 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].

[In Vivo]

Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts[1].

[References]

[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


[Related Small Molecules]

Brigatinib | lorlatinib | Alectinib (CH5424802) | Entrectinib | LOXO-101 | TAE684(NVP-TAE684) | ANA-12 | LM22B 10 | AZD-3463 | GW441756 | Ensartinib | GNF-5837 | AP26113 | K 02288 | ASP3026

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C18H18FN5O2

[ Molecular Weight ]:
355.366

[ Exact Mass ]:
355.144440

[ LogP ]:
1.71

[ Index of Refraction ]:
1.694

[ Storage condition ]:
-20℃

Safety Information

[ Hazard Codes ]:
N

Related Compounds