Cat. No. 3044
Chemical Name: N-[2-[[4-(Diethylamino)butyl]amino]
Biological ActivitySelective FGFR1 and FGFR3 inhibitor (IC50 values are 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively, and > 50000 nM for EGFR, InsR, MEK and PKC). Inhibits VEGF- and FGF-induced angiogenesis in the mouse cornea model of angiogenesis. Inhibits proliferation and differentiation of oligodendrocyte progenitors. Suppresses cell proliferation in cell lines expressing mutated FGFR3 protein. Blocks tumor growth in H510 and H69 SCLC xenograft models.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Miyake et al (2010) 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. 332 795. PMID: 19955487.
Pardo et al (2010) The fibroblast growth factor receptor inhibitor PD173074 blocks small cell lung cancer growth in vitro and in vivo. Cancer Res. 69 8645.
Trudel et al (2004) Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma. Neoplasia 103 3521.
Bansal et al (2003) Specific inhibitor of FGF receptor signaling: FGF-2-mediated effects on proliferation, differentiation, and MAPK activation are inhibited by PD173074 in oligodendrocyte-lineage cells. J.Neurosci.Res. 74 486. PMID: 14598292.
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Citations are publications that use Tocris products. Selected citations for PD 173074 include:
MacKenzie et al (2015) Increased FGF1-FGFRc expression in idiopathic pulmonary fibrosis. Respir Res 16 83. PMID: 26138239.
Saito et al (2015) The role of HGF/MET and FGF/FGFR in fibroblast-derived growth stimulation and lapatinib-resistance of esophageal squamous cell carcinoma. BMC Cancer 15 82. PMID: 25884729.
Witty et al (2014) Generation of the epicardial lineage from human pluripotent stem cells. Nat Biotechnol 32 1026. PMID: 25240927.
Borroto-Escuela et al (2012) The existence of FGFR1-5-HT1A receptor heterocomplexes in midbrain 5-HT neurons of the rat: relevance for neuroplasticity. J Neurosci 32 6295. PMID: 22553035.
Gibson et al (2012) Activation of glial FGFRs is essential in glial migration, proliferation, and survival and in glia-neuron signaling during olfactory system development. PLoS One 7 e33828. PMID: 22493675.
Shifley et al (2012) Prolonged FGF signaling is necessary for lung and liver induction in Xenopus. BMC Dev Biol 12 27. PMID: 22988910.
Wilson et al (2012) Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors. Nature 487 505. PMID: 22763448.
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Keywords: PD 173074, supplier, Selective, FGFR1, FGFR3, inhibitors, inhibits, fibroblast, growth, factors, PD173074, stem, cells, Pfizer, Tocris Bioscience, FGFR Inhibitor products
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