PF-03814735

Bezeichnung:PF-03814735

CAS-Nr942487-16-3

Englisch Name:PF-03814735

CBNumberCB02598705

SummenformelC23H25F3N6O2

Molgewicht474.48

MOL-Datei942487-16-3.mol

PF-03814735 physikalisch-chemischer Eigenschaften

Schmelzpunkt	181-183°C
Dichte	1.443
storage temp.	-20°C
Löslichkeit	DMSO: soluble20mg/mL, clear
Aggregatzustand	powder
pka	15.02±0.46(Predicted)
Farbe	white to beige

Sicherheit

WGK Germany

Gefahreninformationscode (GHS)

PF-03814735 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC₅₀ values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC₅₀ values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC₅₀ values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.
Chemische Eigenschaften
Off-White Solid
Verwenden
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT-116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT-116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.[Cayman Chemical]
Verwenden
PF 03814735 is an orally bioavailable small molecule aurora kinase inhibitor that plays a key role in the regulation of mitosis. PF 03814735 is a anticancer agent used for cancer therapy.
Lager
-20°C
Einzelnachweise
[1] jani jp, arcari j, bernardo v, bhattacharya sk, briere d, cohen bd, coleman k, christensen jg, emerson eo, jakowski a, hook k, los g, moyer jd, pruimboom-brees i, pustilnik l, rossi am, steyn sj, su c, tsaparikos k, wishka d, yoon k, jakubczak jl. pf-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. mol cancer ther. 2010 apr;9(4):883-94.

PF-03814735 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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