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| | 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 | | EINECS: | | | 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. |
| Hazard Codes | Xi | | Risk Statements | 36/37/38 | | Safety Statements | 26-36 | | WGK Germany | 3 |
| | 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A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group.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 |
| | SU 4312 Preparation Products And Raw materials |
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