PD 166285

Bezeichnung:PD 166285

CAS-Nr212391-63-4

Englisch Name:PD 166285

CBNumberCB91873310

SummenformelC26H29Cl4N5O2

Molgewicht585.37

MOL-Datei212391-63-4.mol

PD 166285 physikalisch-chemischer Eigenschaften

Schmelzpunkt	239-242?C
storage temp.	Desiccate at RT
Löslichkeit	DMSO, Methanol
Aggregatzustand	Pale yellow solid
Farbe	Yellow
Stabilität	Hygroscopic

PD 166285 Chemische Eigenschaften,Einsatz,Produktion Methoden

Chemische Eigenschaften
Yellow Solid
Verwenden
A broad-spectrum receptor tyrosine kinase (RTK) inhibitor which shows anti-angiogenic activity and anti-tumor efficacy in combination with photodynamic therapy (PDT).
Allgemeine Beschreibung
A cell-permeable, orally bioavailable, ATP-competitive, broad-spectrum tyrosine kinase inhibitor (IC₅₀ against against c-Src, Wee1, FGFR-1, Myt1, EGFR, and PDGFRβ = 8.4, 24, 39.3, 72, 87.5 and 98.3 nM, respectively) that suppresses angiogenesis both in vitro (max inhibition dose at 100 nM in HUVEC microcapillary formation assays) and in vivo (max inhibition achieved via 5 mg/kg p.o. in murine Matrigel plug angiogenesis assays), while exhibiting much reduced potency against Chk1, MAPK, and PKC (IC₅₀ = 3.4, 5, and 22.7 μM, respectively) and little activity toward IRTK and Cdk4/D1 even at concentrations as high as 50 μM. Shown to effectively block PDGF-, EGF-, and bFGF-stimulated receptor phosphorylations (IC₅₀ = 6.5, 1600, and 97.3 nM, respectively) and other cellular responses in rat aortic smooth muscle cells. Inhibition of cellular Wee1 activity by 500 nM PD 166285 in combination with 50 ng/ml nocodazole (Cat. No. 487928) treatment is also reported to result in a blockage of radiation-induced Cdc2 phosphorylation on Tyr15 and Thr14 in 7 human cancer cells and specifically demonstrated to sensatize PA-1 cultures to radiation-induced cell death in a p53-dependent manner.
Biologische Aktivität
Potent inhibitor of the tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β (PDGFR β ) (IC 50 values are 8.4, 39.3 and 98.3 nM respectively). Also inhibits the checkpoint kinases Wee1 and Myt1; abolishes Cdc2 phosphorylation in numerous tumor cell lines and abrogates the G 2 checkpoint.
Lager
Desiccate at RT

PD 166285 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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