Products & ReviewLife Sciences
SU5416
Tyrosine kinase inhibitor; Inhibits of KDR, PDGFR, KIT, RET, FLT-3, ABL and ALK
SU5416
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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.).
