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PD-166866

Catalog No. T3492 CAS 192705-79-6

Synonyms: PD166866

PD-166866 is a selective FGFR tyrosine kinase inhibitor.

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PD-166866, CAS 192705-79-6

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 55.00
10 mg	In stock	$ 87.00
25 mg	In stock	$ 162.00
50 mg	In stock	$ 321.00
100 mg	In stock	$ 477.00
1 mL * 10 mM (in DMSO)	In stock	$ 56.00

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Purity: 99.98%

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Description	PD-166866 is a selective FGFR tyrosine kinase inhibitor.
Targets&IC50	FGFR1:52.4 nM
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	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.(Only for Reference)

Synonyms	PD166866
Molecular Weight	396.44
Formula	C20H24N6O3
CAS No.	192705-79-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12 mg/mL (30.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 3 mg/mL (7.57 mM)

References and Literature

1. Risuleo G, et al. J Exp Clin Cancer Res. 2009, 28:151. 2. Panek RL, et al. J Pharmacol Exp Ther. 1998, 286(1):569-77. 3. Chen Y, et al. Biochem Biophys Res Commun. 2016, 474(1):1-7.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Target-Focused Phenotypic Screening Library Anti-Prostate Cancer Compound Library Cytokine Inhibitor Library Reprogramming Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

PD-166866 192705-79-6 Angiogenesis Autophagy Tyrosine Kinase/Adaptors FGFR Inhibitor PD166866 PD 166866 inhibit Fibroblast growth factor receptor inhibitor

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