SU 4312
SU 4312 Basic information
- Product Name:
- SU 4312
- Synonyms:
-
- 3-[[(4-DIMETHYLAMINO)PHENYL]METHYLENE]-1,3-DIHYDRO-2H-INDOL-2-ONE
- 3-(4-DIMETHYLAMINOBENZYLIDENYL)-2-INDOLINONE
- 3-[[(4-Dimethylamino)phenyl]methylene]-1,3-dihydro-2H-indol-2-one, E/Z mixture
- NSC 86429
- SU 4312
- 2H-Indol-2-one, 3-[[4-(dimethylamino)phenyl]methylene]-1,3-dihydro
- (Z)-3-(4-(DIMETHYLAMINO)BENZYLIDENE)INDOLIN-2-ONE
- SU4312(NSC86429)
- CAS:
- 5812-07-7
- MF:
- C17H16N2O
- MW:
- 264.32
- Product Categories:
-
- Protein Kinase
- Angiogenesis and Metastasis
- Mol File:
- 5812-07-7.mol
SU 4312 Chemical Properties
- 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.
MSDS
- Language:English Provider:SigmaAldrich
SU 4312 Usage And Synthesis
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A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group.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.
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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