Caractéristiques principales
- 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.)
- 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.)
- Causes pulmonary hypertension in SuHx rat model of pulmonary arterial hypertension, when combined with hypoxia (de Raaf et al.; Mizuno et al.)
- Inhibits TGFβ1 activation and delays wound healing in rats (Haroon et al.)
Caractéristiques techniques
| Marque | STEMCELL Technologies |
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| Réf. B-LABO | BL-RE-158229 |
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| Réf. fabricant | 17170222 |
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| CAS | 204005-46-9 |
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| Synonyme | NSC 696819; Semaxinib; Sugen 5416; VEGFR 2 Kinase Inhibitor |
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| Quantité | 50 mg |
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| Formule moléculaire | C<sub>15</sub>H<sub>14</sub>N<sub>2</sub>O |
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| Pureté | ≥98% |
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