PD-166866

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 has clear antiproliferative effects.

Product information

CAS Number: 192705-79-6

Molecular Weight: 396.44

Formula: C20H24N6O3

Synonym:

PD 166866

PD166866

Chemical Name: 1-(2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)-3-(tert-butyl)urea.

Smiles: CC(C)(C)NC(=O)NC1=NC2=NC(N)=NC=C2C=C1C1C=C(C=C(C=1)OC)OC

InChiKey: NHJSWORVNIOXIT-UHFFFAOYSA-N

InChi: InChI=1S/C20H24N6O3/c1-20(2,3)26-19(27)25-17-15(8-12-10-22-18(21)24-16(12)23-17)11-6-13(28-4)9-14(7-11)29-5/h6-10H,1-5H3,(H4,21,22,23,24,25,26,27)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 14 mg/mLwarmed(35.31 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

PD-166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC50 value of 52.4 nM and is characterized as an ATP competitive inhibitor of the FGFR-1. PD-166866 is a potent inhibitor of FGFR autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase. PD-166866 also inhibits bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms in L6 cells. Daily exposure of PD-166866 to L6 cells at concentrations from 1 to 100 nM results in a concentration-related inhibition of bFGF-stimulated cell growth for 8 consecutive days with an IC50 value of 24 nM.

References:

1. Murayama N, Kadoshima T, Takemoto N, Kodama S, Toba T, Ogino R, Noshita T, Oka T, Ueno S, Kuroda M, Shimmyo Y, Morita Y, Inoue T. SUN11602, a novel aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor. ACS Chem Neurosci. 2013 Feb 20;4(2):266-76. doi: 10.1021/cn300183k. Epub 2012 Nov 21. PubMed PMID: 23421678; PubMed Central PMCID: PMC3582292.
2. Risuleo G, Ciacciarelli M, Castelli M, Galati G. The synthetic inhibitor of fibroblast growth factor receptor PD166866 controls negatively the growth of tumor cells in culture. J Exp Clin Cancer Res. 2009 Dec 11;28:151. doi: 10.1186/1756-9966-28-151. PubMed PMID: 20003343; PubMed Central PMCID: PMC2797793.
3. Ohshima M, Yamaguchi Y, Kappert K, Micke P, Otsuka K. bFGF rescues imatinib/STI571-induced apoptosis of sis-NIH3T3 fibroblasts. Biochem Biophys Res Commun. 2009 Apr 3;381(2):165-70. doi: 10.1016/j.bbrc.2009.02.012. Epub 2009 Feb 10. PubMed PMID: 19338769.

Products are for research use only. Not for human use.