| Identification | Back Directory | [Name]
SU 4312 | [CAS]
5812-07-7 | [Synonyms]
SU 4312
NSC 86429
SU4312(NSC86429)
SU 4312;NSC 86429;SU-4312;NSC-86429
3-(4-DIMETHYLAMINOBENZYLIDENYL)-2-INDOLINONE
(Z)-3-(4-(DIMETHYLAMINO)BENZYLIDENE)INDOLIN-2-ONE
3-[[(4-DIMETHYLAMINO)PHENYL]METHYLENE]-1,3-DIHYDRO-2H-INDOL-2-ONE
2H-Indol-2-one, 3-[[4-(dimethylamino)phenyl]methylene]-1,3-dihydro
3-[[(4-Dimethylamino)phenyl]methylene]-1,3-dihydro-2H-indol-2-one, E/Z mixture | [Molecular Formula]
C17H16N2O | [MDL Number]
MFCD00118147 | [MOL File]
5812-07-7.mol | [Molecular Weight]
264.32 |
| Chemical Properties | Back Directory | [Melting point ]
225-232 °C | [Boiling point ]
497.1±45.0 °C(Predicted) | [density ]
1.219±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C
| [solubility ]
DMSO: 30 mg/mL
| [form ]
Orange solid. | [pka]
12.89±0.20(Predicted) | [color ]
orange
| [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
SU-4312 (5812-07-7) is a potent selective inhibitor of VEGFR kinase (also known as Flk-1 and KDR). Inhibition of the activated kinase (IC50 = 0.4 μM) is 100-fold less than inhibition of the unactivated kinase (IC50 = 0.04 μM). SU-4312 also inhibits PDGFR kinase (IC50 = 19.4 μM). | [Uses]
SU 4312 is a vascular endothelial growth factor receptor KDR tyrosine kinase antagonist. | [Definition]
ChEBI: A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group. SU 4312 is a vascular endothelial growth factor (VEGF) receptor protein
yrosine kinase 1/2 and platelet derived growth factor (PDGF) receptor inhibitor. It also inhibits the neuronal nitric oxide synthase (NOS) and exhibits neuroprotection against NO-mediated neurotoxicity. | [Biological Activity]
Potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC 50 values are 0.8 and 19.4 mM respectively). Selective over EGFR and c-Src tyrosine kinases. | [IC 50]
PDGFR; Flk-1 | [storage]
Desiccate at -20°C,unstable in solution, ready to use. | [References]
1) Kendall et al. (1999), Vascular endothelial growth factor receptor KDR tyrosine kinase activity is increased by autophosphorylation of two activation loop tyrosine residues; J. Biol. Chem., 274 6453
2) Sun et al. (1998), Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases; J. Med. Chem., 41 2588 |
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