Repotrectinib


CAS No. : 1802220-02-5

(Synonyms: TPX-0005)

1802220-02-5
Price and Availability of CAS No. : 1802220-02-5
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5mg $132 In-stock
10mg $210 In-stock
25mg $420 In-stock
50mg $649 In-stock
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Cat. No. : HY-103022
M.Wt: 355.37
Formula: C18H18FN5O2
Purity: >98 %
Solubility: DMSO : 25 mg/mL (ultrasonic)
Introduction of 1802220-02-5 :

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]. IC50 & Target:IC50: 0.07 nM (ROS1), 0.83/0.05/0.1 nM (TRKA/B/C), 1.01 nM (ALK), 1.04 nM (JAK2), 1.66 nM (LYN), 5.3 nM (Src), 6.96 nM (FAK)[1][2] In Vitro: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]. In Vivo:Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts[1].

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