Dovitinib

Bezeichnung:Dovitinib

CAS-Nr915769-50-5

Englisch Name:Dovitinib

CBNumberCB31518505

SummenformelC24H29FN6O5

Molgewicht500.5226632

MOL-Datei915769-50-5.mol

Dovitinib physikalisch-chemischer Eigenschaften

storage temp.	Store at -20°C
Löslichkeit	insoluble in EtOH; ≥10.62 mg/mL in DMSO; ≥168.2 mg/mL in H2O
Aggregatzustand	Powder

Gefahreninformationscode (GHS)

Dovitinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hydroxypropanoate hydrate is a useful research chemical compound.
Biologische Aktivität
fibroblast growth factor receptor 1 (fgfr1) and fgfr2 amplifications are observed in approximately 10% of breast cancers and are related to poor outcomes. dovitinib (tki258) is an oral tyrosine kinase inhibitor (tki) against fgfr1–3, vegfr1–3, and platelet-derived growth factor receptor (pdgfr).
in vitro
dovitinib decreased the concentrations of pfrs2 and perk/mapk in a dose-dependent manner in fgfr1 amplified and fgfr2 amplified cell lines. the ic50 for cell growth inhibition was 190 and 180 nmol/l in mda-mb-134 and sum52, respectively. conversely, ic50 values were more than 2,000 nmol/l in the 11 breast cancer cell lines that had neither fgfr1 nor fgfr2 amplification [1].
in vivo
in vivo model (hbcx-2 breast cancer primary xenograft, with 8 fgfr1 gene copies), dovitinib prevented tumor growth at the 30 mg/kg dose and caused tumor regression at the 50 mg/kg dose. similarly, dovitinib caused tumor regression in hbcx-3 xenografts when administered at a dose of 40 mg/kg daily until day 35 [1].
IC 50
~10 nmol/l for fgfr1–3
Einzelnachweise
[1] andré f, bachelot t, campone m, dalenc f, perez-garcia jm, hurvitz sa, turner n, rugo h, smith jw, deudon s, shi m, zhang y, kay a, porta dg, yovine a, baselga j. targeting fgfr with dovitinib (tki258): preclinical and clinical data in breast cancer. clin cancer res. 2013 jul 1;19(13):3693-702.

Dovitinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

915769-50-5, Dovitinib Verwandte Suche:

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