MedKoo Biosciences

PD166866
featured

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.

Chemical Structure

PD166866

CAS# 192705-79-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406475
Name: PD166866
CAS#: 192705-79-6
Chemical Formula: C20H24N6O3
Exact Mass: 396.19
Molecular Weight: 396.443
Elemental Analysis: C, 60.59; H, 6.10; N, 21.20; O, 12.11

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 150
25mg	USD 250
50mg	USD 450
100mg	USD 750
200mg	USD 1050
500mg	USD 1950
1g	USD 2950
2g	USD 4650
5g	USD 7850
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.
In vitro activity:	PD 166866 was 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 also inhibited bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms in L6 cells, presumably via inhibition of bFGF-stimulated FGFR-1 tyrosine kinase activation. Reference: J Pharmacol Exp Ther. 1998 Jul;286(1):569-77. https://pubmed.ncbi.nlm.nih.gov/9655904/
In vivo activity:	TBD

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	2.0	5.04
	DMF:PBS (pH 7.2) (1:6)	0.1	0.35
	DMSO	3.5	8.83
	Ethanol	0.1	0.25

Preparing Stock Solutions

The following data is based on the product molecular weight 396.443000000000000000000000000000 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

Formulation protocol:	1. Chen Y, Xie X, Li X, Wang P, Jing Q, Yue J, Liu Y, Cheng Z, Li J, Song H, Li G, Liu R, Wang J. FGFR antagonist induces protective autophagy in FGFR1-amplified breast cancer cell. Biochem Biophys Res Commun. 2016 May 20;474(1):1-7. doi: 10.1016/j.bbrc.2016.03.017. Epub 2016 Mar 16. PMID: 26993162. 2. Panek RL, Lu GH, Dahring TK, Batley BL, Connolly C, Hamby JM, Brown KJ. In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase. J Pharmacol Exp Ther. 1998 Jul;286(1):569-77. PMID: 9655904.
In vitro protocol:	1. Chen Y, Xie X, Li X, Wang P, Jing Q, Yue J, Liu Y, Cheng Z, Li J, Song H, Li G, Liu R, Wang J. FGFR antagonist induces protective autophagy in FGFR1-amplified breast cancer cell. Biochem Biophys Res Commun. 2016 May 20;474(1):1-7. doi: 10.1016/j.bbrc.2016.03.017. Epub 2016 Mar 16. PMID: 26993162. 2. Panek RL, Lu GH, Dahring TK, Batley BL, Connolly C, Hamby JM, Brown KJ. In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase. J Pharmacol Exp Ther. 1998 Jul;286(1):569-77. PMID: 9655904.
In vivo protocol:	TBD

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

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-VÃ¶rÃ¶smarty 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, EstÃ©vez 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.

Your view history

PD166866 featured