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ChemicalBook--->CAS DataBase List--->5812-07-7

5812-07-7

5812-07-7 Structure

5812-07-7 Structure
IdentificationBack 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 PropertiesBack 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.
Safety DataBack Directory
[Hazard Codes ]

Xi
[Risk Statements ]

36/37/38
[Safety Statements ]

26-36
[WGK Germany ]

3
Hazard InformationBack 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A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group.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.
[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
Spectrum DetailBack Directory
[Spectrum Detail]

SU 4312(5812-07-7)1HNMR
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