Formulation: A crystalline solid
Formal Name: 6-[[7-[(1-aminocyclopropyl)methoxy]-6-methoxy-4-quinolinyl]oxy]-N-methyl-1-naphthalenecarboxamide, dihydrochloride
Purity: ≥95%
Formula Markup: C26H25N3O4 • 2HCl
CAS Number: 2108875-91-6
Notes: Lucitanib is a dual inhibitor of VEGFR and FGFR that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50s = 7, 25, and 10 nM, respectively) and FGFR1 and FGFR2 (IC50s = 17.5 and 82.5 nM, respectively).{66808} It is selective for these receptors over FGFR3 and FGFR4 (IC50s = 237.5 and >1,000 nM, respectively), as well as the PDGFR family members c-Kit, PDGFRα, and PDGFRβ (IC50s = 456, 175, and 525 nM, respectively), but does inhibit FMS, also known as CSF-1 receptor tyrosine kinase (IC50 = 5 nM). Lucitanib inhibits the proliferation of human umbilical vein endothelial cells (HUVECs) induced by VEGF or basic FGF (bFGF; IC50s = 40 and 50 nM, respectively) but inhibits the proliferation of A2780 ovarian, A498 renal, and SN12KI renal cancer cells only at higher concentrations (IC50s = 27.7, 19.6, and 12.79 µM, respectively). It reduces tumor growth in HT-29 colon and A2780 ovarian cancer mouse xenograft models, as well as in RXF 393, A498, and SKN12I renal cancer mouse xenograft models in a dose-dependent manner. It also completely inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice when administered at a dose of 20 mg/kg.
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