Home Angiogenesis FGFR inhibitor PD-166866 For research use only.

PD-166866

PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1.

PD-166866 Chemical Structure

PD-166866 Chemical Structure

CAS No. 192705-79-6

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PD-166866 Related Products

Signaling Pathway

FGFR Signaling Pathways

FGFR Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC cells Function assay Inhibition of microcapillary growth in HUVEC cells, IC50=0.1 μM 11063616
Click to View More Cell Line Experimental Data

Biological Activity

Description PD-166866 is a synthetic molecule inhibiting the tyrosin kinase action of FGFR1, shows a very high selectivity towards FGFR1 and inhibits the auto-phosphorylation activity of FGRF1.
Targets
FGFR1 [2]
(Cell-free assay)
52.4 nM
In vitro
In vitro The treatment with PD166866 apparently causes a mitochondrial deficit and an oxidative stress[1]. PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC50 value of 52.4 ± 0.1 nM but has no effect on c-Src, platelet-derived growth factor receptor-β, epidermal growth factor receptor or insulin receptor tyrosine kinases or on mitogen-activated protein kinase, protein kinase C and CDK4 at concentrations as high as 50 μM. PD 166866 is a potent inhibitor of basic fibroblast growth factor (bFGF)-mediated receptor autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase, confirming a tyrosine kinase-mediated mechanism. PD 166866 does not inhibit platelet-derived growth factor, epidermal growth factor or insulin-stimulated receptor autophosphorylation in vascular smooth muscle, A431 or NIHIR cells, respectively, further supporting its specificity for the FGFR-1. Besides, PD 166866 is found to be a potent inhibitor of microvessel outgrowth (angiogenesis) from cultured artery fragments of human placenta. Phosphorylated 44- and 42-kDa MAPK isoforms are inhibited in L6 cells by PD 166866 with IC50 values of 4.3 and 7.9 nM, respectively[2]. PD166866 induces autophagy through repressing Akt/mTOR signaling pathway[3].
Cell Research Cell lines HeLa cells
Concentrations 50 μM
Incubation Time 24 h
Method HeLa cells are treated with PD166866 for 24 hours, the growth medium is removed, the cells are washed with PBS and fixed for 1 hour at 25°C adding a freshly made paraformaldheyde solution (4% in PBS). Samples are washed again with PBS and the endogenous oxidases were blocked for 2 minutes in the dark. Further washes with PBS followed and blocking the unspecific sites is done for 1 hour at 25℃. PARP is evidenced by immunolocalization utilizing a polyclonal antibody, directed against the N-terminal proteolytic fragment. Immuno-reaction is revealed by a secondary anti-rabbit antibody after incubation for 16 hours at 4°C. After exhaustive washing with PBS the samples are incubated for 30 minutes in solution ABC. Eventually, DAB (3,3'-Diaminobenzidine) is added and the samples are incubated for 10 minutes in the dark. The samples are washed again the plates are sealed and ready for microscopic observation.

Chemical Information & Solubility

Molecular Weight 396.44 Formula

C20H24N6O3
CAS No. 192705-79-6 SDF Download PD-166866 SDF
Smiles CC(C)(C)NC(=O)NC1=C(C=C2C=NC(=NC2=N1)N)C3=CC(=CC(=C3)OC)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 40 mg/mL ( (100.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

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