OSI-930

Bezeichnung:OSI-930

CAS-Nr728033-96-3

Englisch Name:OSI-930

CBNumberCB52512522

SummenformelC22H16F3N3O2S

Molgewicht443.44

MOL-Datei728033-96-3.mol

OSI-930 physikalisch-chemischer Eigenschaften

Siedepunkt	517.4±50.0 °C(Predicted)
Dichte	1.450
storage temp.	Store at -20°C
Löslichkeit	≥22.15 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
pka	11.36±0.70(Predicted)
Aggregatzustand	solid

Gefahreninformationscode (GHS)

OSI-930 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
OSI-930 is an inhibitor of the receptor tyrosine kinases c-Kit (IC50:9.5nM) and VEGFR-2 (IC50:10.1nM).
Definition
ChEBI: 3-(4-quinolinylmethylamino)-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide is an aromatic amide.
Biologische Aktivität
osi-930 is a novel, potent inhibitor of flt1, kinase insert domain receptor (kdr), csf-1r, lck, c-raf and activated receptor tyrosine kinases kit with ic50 values of 8, 9, 15, 22, 41 and 80 nm, respectively [1].osi-930 has been demonstrated to inhibit proliferation and induce apoptosis in the hmc-1 cell line which is highly dependent on kit signaling for survival. on the contrary, osi-930 revealed no growth inhibition of colo-205 cell line under normal culture conditions [1].osi-930 has shown to time- and concentration-dependently inactivate p450 3a4. additionally, osi-930 could reduce co difference spectra of p450 3a4 [2].
target
c-Kit
Einzelnachweise
[1] garton aj1, crew ap, franklin m, cooke ar, wynne gm, castaldo l, kahler j, winski sl, franks a, brown en, bittner ma, keily jf, briner p, hidden c, srebernak mc, pirrit c, o'connor m, chan a, vulevic b,henninger d, hart k, sennello r, li ah, zhang t, richardson f, emerson dl, castelhano al, arnold ld,gibson nw. osi-930: a novel selective inhibitor of kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. cancer res. 2006 jan 15;66(2):1015-24.
[2] lin hl1, zhang h, medower c, hollenberg pf, johnson ww. inactivation of cytochrome p450 (p450) 3a4 but not p450 3a5 by osi-930, a thiophene-containing anticancer drug. drug metab dispos. 2011 feb;39(2):345-50.

OSI-930 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

728033-96-3, OSI-930 Verwandte Suche:

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