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| Cas No.: | 1802220-02-5 |
| Chemical Name: | Repotrectinib |
| Synonyms: | TPX-0005;Repotrectinib;Ropotrectinib;08O3FQ4UNP;Repotrectinib (USAN);Repotrectinib [USAN];GTPL10316;TPX0005;TPX 0005 [WHO-DD];BDBM374727;US10246466 |
| SMILES: | FC1C=CC2=C(C=1)[C@@H](C)NC1C=CN3C(=C(C=N3)C(NC[C@H](C)O2)=O)N=1 |
| Formula: | C18H18FN5O2 |
| M.Wt: | 355.3662 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| 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. |
| In Vivo: | Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts[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]. |