102586-30-1

NSC12 (NSC 172285) is an orally available inhibitor of FGF2/FGFR interaction with potential antitumor activity.

NSC-12 can inhibit FGF-dependent tumor growth, angiogenesis and metastasis. It did not affect FGF2/heparin interaction, but inhibited FGF2 binding to immobilized receptors (IC50 ~30 μM), it disrupted FGF2 interaction with FGFR1, and had no effect on the interaction activity of growth factors with heparin or HSPGs .

Administered by injection and oral route, NSC-12 inhibits FGFR activation, tumor growth, angiogenesis and metastasis in FGF-dependent mouse and human tumor models. In animal models, it significantly reduced tumor weight, tumor cell FGFR1 phosphorylation levels and proliferation, and tumor CD31+ cardiovascular formation.

Target	Value
FGF3 (Cell-free assay)	15.9 μM(Kd)
FGF8b (Cell-free assay)	18.9 μM(Kd)
FGF22 (Cell-free assay)	26.8 μM(Kd)
FGF20 (Cell-free assay)	29.4 μM(Kd)
FGF2/FGFR (Cell-free assay)	30 μM

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