LY 2874455

Bezeichnung:LY 2874455

CAS-Nr1254473-64-7

Englisch Name:LY 2874455

CBNumberCB12616026

SummenformelC21H19Cl2N5O2

Molgewicht444.31

MOL-Datei1254473-64-7.mol

LY 2874455 physikalisch-chemischer Eigenschaften

Siedepunkt	672.6±55.0 °C(Predicted)
Dichte	1.44
storage temp.	Store at -20°C
Löslichkeit	≥44.4 mg/mL in DMSO; insoluble in H2O; ≥6.34 mg/mL in EtOH with gentle warming and ultrasonic
Aggregatzustand	solid
pka	12.93±0.40(Predicted)
Farbe	Pink to gray
CAS Datenbank	1254473-64-7

Gefahreninformationscode (GHS)

LY 2874455 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
LY 2874455 is a pan-FGFR inhibitor which remain the focus of research for use in lung and bladder cancers.
Biologische Aktivität
ly2874455 is a novel and potent fgfr inhibitor with ic50 value of 7 nm [1].fibroblast growth factor receptors (fgfrs) are receptors bind ligand of fgf family, which have a intracellular domain with tyrosine kinase activity. the binding of fgf triggers receptor dimerization and thus the activation of tyrosine kinase activity. activated tyrosine kinase phosphorylates various downstream factors to induce downstream signaling, including fgf substrate 2 (fgs2). this signaling pathway contributes to fgfr-mediated cell proliferation and migration, which are involved in tumor formation and progression.in huvecs cell line expressing fgfr1 and rt-112 cell line expressing fgfr3, ly2874455 treatment resulted in inhibition of fgf2 and fgf9 induced erk phosphorylation, which indicated the inhibitory activity of ly2874455 for fgfr1 and fgfr3 [1]. in snu-16 and kato-ш cell line, the inhibition of fgfr2 phosphorylation was also observed, which indicated a direct inhibition by ly2874455 [2]. additionally, when several multiple myeloma cancer cell lines were treated with lys2874455, the cell lines with chromosomal translocation that resulted in overexpression of fgfr3 were significantly more susceptible to the inhibition of ly2874455 [2]. it suggested fgfr was the specific target of ly2874455 inhibition.in rt-112, snu-16, opm-2 and nci-h460 xenograft tumor model, treatment of ly2874455 twice a day (1.5 mg/kg and 3 mg/kg) resulted in significant dose-dependent reduction of cellular level of phosphorylated fgfr, and also regression of tumor growth. it indicated the inhibitory activity of ly2874455 in vivo [2].
target
FGFR1
Einzelnachweise
[1] zhao, g s et al. , a novel, selective inhibitor of fibroblast growth factor receptors that shows a potent broad spectrum of antitumor activity in several tumor xenograft models. molecular cancer therapeutics. 2011, 10(11): 2200-2210.

LY 2874455 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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