PD-166866


Catalog No. size PriceQuantity
M6541-2 2mg solid $90
M6541-10 10mg solid $371

Description

Cas:192705-79-6

Product Information:

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. PD166866 has clear antiproliferative effects.

 

Chemical Formula: C20H24N6O3

 

Exact Mass: 396.19099

 

Molecular Weight: 396.44296

 

Elemental Analysis: C, 60.59; H, 6.10; N, 21.20; O, 12.11

 

Synonym:

 

PD166866

PD166866

PD 166866

 

Chemical Name: 

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

 

InChi Key:

NHJSWORVNIOXIT-UHFFFAOYSA-N

 

InChi Code: 

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)

 

Smiles Code:

O=C(NC(C)(C)C)NC1=NC2=NC(N)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3

 

 

Technical Data:

 

Appearance: white solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

 

  1. 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.

 

  1. 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.

 

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