PD 166866 Struktur

PD 166866

Bezeichnung:PD 166866

CAS-Nr192705-79-6

Englisch Name:PD 166866

CBNumberCB42485694

SummenformelC20H24N6O3

Molgewicht396.44

MOL-Datei192705-79-6.mol

PD 166866 physikalisch-chemischer Eigenschaften

Schmelzpunkt	291-293°C
storage temp.	2-8°C
Löslichkeit	DMSO: ≥10mg/mL
Aggregatzustand	Off-white solid
Farbe	off-white to light tan

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
WGK Germany	1

Gefahreninformationscode (GHS)

PD 166866 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
PD 166866 is a potent inhibitor of fibroblast growth factor receptor 1 (FGFR1; IC₅₀ = 52.4 nM; K_i = 45.2 nM). It is selective for FGFR1 over PDGFR, EGFR, C-SRC, MEK, PKC, insulin receptor tyrosine kinase, and CDK4 (IC₅₀s = >50 μM). PD 166866 inhibits FGFR1 autophosphorylation in NIH3T3 and L6 cells (IC₅₀s = 10.8 and 3.1 nM, respectively) and inhibits phosphorylation of MAPK (IC₅₀s = 4.3 and 7.9 nM for the 44- and 42-kDa MAPK isoforms, respectively). It reduces FGF- but not EGF- or PDGF-stimulated growth of L6 cells and inhibits microvessel outgrowth from human placental arteries in vitro. PD 166866 inhibits the growth of non-small cell lung cancer (NSCLC) cell lines in a dose-dependent manner and reduces migration of VL-8 cells at a concentration of 10 μM.
Chemische Eigenschaften
Off-White Solid
Verwenden
A novel potent ATP competitive pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. An inhibitor of the basic fibroplast growth factor (bFGF).
Definition
ChEBI: PD-166866 is a member of the class of pyridopyrimidines that is pyrido[2,3-d]pyrimidine substituted by an amino group at position 2, 3,5-dimethoxyphenyl group at position 6, and by a (tert-butylcarbamoyl)nitrilo group at position 7. It is a selective ATP competitive inhibitor of the human fibroblast growth factor-1 receptor (FGFR1) tyrosine kinase with an IC50 of 52.4 nM. It has a role as an apoptosis inducer, an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an angiogenesis inhibitor. It is a dimethoxybenzene, a pyridopyrimidine, a member of ureas, a biaryl and a primary arylamine.
Biochem/physiol Actions
PD-166866 is a selective inhibitor of the FGF-1 receptor tyrosine kinase (FGFR1) with IC50 = 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.

PD 166866 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Send Inquriy