WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406475
CAS#: 192705-79-6
Description: PD166866 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.
MedKoo Cat#: 406475
Name: PD166866
CAS#: 192705-79-6
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.
IUPAC/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
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
The following data is based on the product molecular weight 396.44296 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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: Metzner T, Bedeir A, Held G, Peter-Vörösmarty B, Ghassemi S, Heinzle C, Spiegl-Kreinecker S, Marian B, Holzmann K, Grasl-Kraupp B, Pirker C, Micksche M, Berger W, Heffeter P, Grusch M. Fibroblast growth factor receptors as therapeutic targets in human melanoma: synergism with BRAF inhibition. J Invest Dermatol. 2011 Oct;131(10):2087-95. doi: 10.1038/jid.2011.177. Epub 2011 Jul 14. PubMed PMID: 21753785; PubMed Central PMCID: PMC3383623.
3: 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.
4: 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.
5: Fischer H, Taylor N, Allerstorfer S, Grusch M, Sonvilla G, Holzmann K, Setinek U, Elbling L, Cantonati H, Grasl-Kraupp B, Gauglhofer C, Marian B, Micksche M, Berger W. Fibroblast growth factor receptor-mediated signals contribute to the malignant phenotype of non-small cell lung cancer cells: therapeutic implications and synergism with epidermal growth factor receptor inhibition. Mol Cancer Ther. 2008 Oct;7(10):3408-19. doi: 10.1158/1535-7163.MCT-08-0444. PubMed PMID: 18852144; PubMed Central PMCID: PMC2879863.
6: Calandrella N, Risuleo G, Scarsella G, Mustazza C, Castelli M, Galati F, Giuliani A, Galati G. Reduction of cell proliferation induced by PD166866: an inhibitor of the basic fibroblast growth factor. J Exp Clin Cancer Res. 2007 Sep;26(3):405-9. PubMed PMID: 17987803.
7: Piccioni F, Borioni A, Delfini M, Del Giudice MR, Mustazza C, Rodomonte A, Risuleo G. Metabolic alterations in cultured mouse fibroblasts induced by an inhibitor of the tyrosine kinase receptor Fibroblast Growth Factor Receptor 1. Anal Biochem. 2007 Aug 1;367(1):111-21. Epub 2007 Apr 12. PubMed PMID: 17512489.
8: Cassina P, Pehar M, Vargas MR, Castellanos R, Barbeito AG, Estévez AG, Thompson JA, Beckman JS, Barbeito L. Astrocyte activation by fibroblast growth factor-1 and motor neuron apoptosis: implications for amyotrophic lateral sclerosis. J Neurochem. 2005 Apr;93(1):38-46. PubMed PMID: 15773903.
9: Patel NG, Kumar S, Eggo MC. Essential role of fibroblast growth factor signaling in preadipoctye differentiation. J Clin Endocrinol Metab. 2005 Feb;90(2):1226-32. Epub 2004 Nov 2. PubMed PMID: 15522930.
10: Stevens DA, Harvey CB, Scott AJ, O'Shea PJ, Barnard JC, Williams AJ, Brady G, Samarut J, Chassande O, Williams GR. Thyroid hormone activates fibroblast growth factor receptor-1 in bone. Mol Endocrinol. 2003 Sep;17(9):1751-66. Epub 2003 Jun 12. PubMed PMID: 12805413.
11: Li G, Oparil S, Kelpke SS, Chen YF, Thompson JA. Fibroblast growth factor receptor-1 signaling induces osteopontin expression and vascular smooth muscle cell-dependent adventitial fibroblast migration in vitro. Circulation. 2002 Aug 13;106(7):854-9. PubMed PMID: 12176960.
