SU 4312 Struktur

SU 4312

Bezeichnung:SU 4312

CAS-Nr5812-07-7

Englisch Name:SU 4312

CBNumberCB0444460

SummenformelC17H16N2O

Molgewicht264.32

MOL-Datei5812-07-7.mol

SU 4312 physikalisch-chemischer Eigenschaften

Schmelzpunkt	225-232 °C
Siedepunkt	497.1±45.0 °C(Predicted)
Dichte	1.219±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: 30 mg/mL
Aggregatzustand	Orange solid.
pka	12.89±0.20(Predicted)
Farbe	orange
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-36
WGK Germany	3

Gefahreninformationscode (GHS)

SU 4312 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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).
Verwenden
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A member of the class of oxindoles that is 3-methyleneoxindole in which one of the hydrogens of the methylene group has been replaced by a p-(dimethylamino)phenyl group.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.
Biologische Aktivität
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.
Einzelnachweise
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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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