SU5416​

SU5416 is a tyrosine kinase inhibitor best known as an ATP-competitive inhibitor of the kinase insert domain (KDR/VEGFR2/FLK1). In addition to inhibiting KDR (IC₅₀ = 1 μM), SU5416 also inhibits PDGFR (IC₅₀ = 20 μM), KIT (IC₅₀ = 30 nM), RET (IC₅₀ = 170 nM), FLT-3 (IC₅₀ = 160 nM), ABL (IC₅₀ = 11 μM), and ALK (IC₅₀ = 1.2 μM). SU5416 does not inhibit EGFR or FGFR tyrosine kinases (IC₅₀ > 100 μM; Fong et al.; Litz; Mologni et al.).

CANCER RESEARCH

• Prevents angiogenesis, thereby inhibiting tumor growth, catalysis and vascularization for a variety of cancers (Litz; Fong et al.).
• Inhibits RET-mediated transformation of NIH-3T3 mouse fibroblasts and Ba/F3 mouse pro-B cells (Mologni et al.).

DISEASE MODELING

• Causes pulmonary hypertension in SuHx rat model of pulmonary arterial hypertension, when combined with hypoxia (de Raaf et al.; Mizuno et al.).

IMMUNOLOGY

• Inhibits TGFβ1 activation and delays wound healing in rats (Haroon et al.).