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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). PX-0005 inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib.
In vivo: Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts.
Molecular Weight | 355.37 |
Formula | C18H18FN5O2 |
CAS Number | 1802220-02-5 |
Solubility (25°C) | 83 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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TL13-22
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TL13-110
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NVL-655 TFA
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