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PDGFR&FGFR

PD173074 (219580-11-7)

PD173074 is a member of the class of ureas that is 1-tert-butylurea in which one of the hydrogens attached to N(3) is substituted by a pyrido[2,3-d]pyrimidin-7-yl group, which is itself substituted at positions 2 and 6 by a 4-(diethylamino)butyl]amino group and a 3,5-dimethoxyphenyl group, respectively.

Not Intended for Therapeutic Use. For research use only.

CAS: 219580-11-7 Category

PD173074 (219580-11-7) Description:

PD173074 is a small-molecule FGFR3-selective tyrosine kinase inhibitor (TKI), as a therapeutic modality using eight UC cell lines. PD173074 suppressed cell proliferation remarkably in two cell lines, namely, UM-UC-14 and MGHU3, which expressed mutated FGFR3 protein. Cell cycle analysis revealed the growth inhibitory effect of PD173074 was associated with arrest at G(1)-S transition in a dose-depending manner. In the mouse xenograft models using subcutaneously transplanted UM-UC-14 and MGHU3, orally administered PD173074 suppressed tumor growth and induced apoptotic changes comparable with the results of our in vitro assay.

PD173074 (219580-11-7) Specifications:

Product Name PD173074
Synonym PD173074; PD 173074; PD-173074.
Chemical Name 1-(tert-butyl)-3-(2-((4-(diethylamino)butyl)amino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)urea
Purity ≥98% (HPLC)
CAS Number 173074
Molecular Formula C28H41N7O3
Molecular Weight 523.682 g/mol
Monoisotopic Mass 523.327 g/mol
MDL number MFCD08705327
InChIKey DXCUKNQANPLTEJ-UHFFFAOYSA-N
InChi Code InChI=1S/C28H41N7O3/c1-8-35(9-2)13-11-10-12-29-26-30-18-20-16-23(19-14-21(37-6)17-22(15-19)38-7)25(31-24(20)32-26)33-27(36)34-28(3,4)5/h14-18H,8-13H2,1-7H3,(H3,29,30,31,32,33,34,36)
SMILES O=C(NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3)NC(C)(C)C
Form Powder
Color yellow
Solubility  DMSO: 10 mg/mL, clear
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application small-molecule FGFR3-selective tyrosine kinase inhibitor (TKI)

 


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RIDADR NONH for all modes of transport

References:

[1]. Dimitroff CJ, Klohs W, Sharma A, Pera P, Driscoll D, Veith J, Steinkampf R, Schroeder M, Klutchko S, Sumlin A, Henderson B, Dougherty TJ, Bernacki RJ. Anti-angiogenic activity of selected receptor tyrosine kinase inhibitors, PD166285 and PD173074: implications for combination treatment with photodynamic therapy. Invest New Drugs. 1999;17(2):121-35. PubMed PMID: 10638483.,

[2]. Lysosomal Sequestration Impairs the Activity of the Preclinical FGFR Inhibitor PD173074. Englinger B, Kallus S, Senkiv J, Laemmerer A, Moser P, Gabler L, Groza D, Kowol CR, Heffeter P, Grusch M, Berger W.Cells. 2018 Dec 8;7(12). pii: E259. doi: 10.3390/cells7120259.PMID: 30544798

[3].  NMR backbone assignments of the tyrosine kinase domain of human fibroblast growth factor receptor 3 in apo state and in complex with inhibitor PD173074.Sanfelice D, Koss H, Bunney TD, Thompson GS, Farrell B, Katan M, Breeze AL.Biomol NMR Assign. 2018 Oct;12(2):231-235. doi: 10.1007/s12104-018-9814-7. Epub 2018 Mar 26.PMID: 29582384

[4]. Miyake M, Ishii M, Koyama N, Kawashima K, Kodama T, Anai S, Fujimoto K, Hirao Y, Sugano K. 1-tert-butyl-3-[6-(3,5-dimethoxy-phenyl)-2-(4-diethylamino-butylamino)-pyrido[2,3 -d]pyrimidin-7-yl]-urea (PD173074), a selective tyrosine kinase inhibitor of fibroblast growth factor receptor-3 (FGFR3), inhibits cell proliferation of bladder cancer carrying the FGFR3 gene mutation along with up-regulation of p27/Kip1 and G1/G0 arrest. J Pharmacol Exp Ther. 2010 Mar;332(3):795-802. doi: 10.1124/jpet.109.162768. Epub 2009 Dec 2. PubMed PMID: 19955487

[5]. Byron SA, Chen H, Wortmann A, Loch D, Gartside MG, Dehkhoda F, Blais SP, Neubert TA, Mohammadi M, Pollock PM. The N550K/H mutations in FGFR2 confer differential resistance to PD173074, dovitinib, and ponatinib ATP-competitive inhibitors. Neoplasia. 2013 Aug;15(8):975-88. PubMed PMID: 23908597; PubMed Central PMCID: PMC3730048

1 review for PD173074 (219580-11-7)

  1. Cofttek

    Never had such good experience before,The PD173074 (219580-11-7) is high purity,also customer service is pretty nice !gotta try!!

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