Home / FGF Receptor Inhibitors / PD 173074

PD 173074

Catalog #: 3044
20 Citations Datasheet / COA / SDS
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PD 173074 | CAS No. 219580-11-7 | FGF Receptor Inhibitors
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Description: FGFR1 and -3 inhibitor

Chemical Name: N-[2-[[4-(Diethylamino)butyl]amino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)urea

Purity: ≥98%

Product Details
Citations (20)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

PD 173074 is a selective 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. Also promotes mESC self-renewal, facilitates the conversion of mouse epiblast stem cells to an earlier pluripotency state and inhibits differentiation of miPSCs to cardiomyocytes. Suppresses cell proliferation in cell lines expressing mutated FGFR3 protein. Blocks tumor growth in H510 and H69 SCLC xenograft models.

Technical Data

M.Wt:
523.67
Formula:
C28H41N7O3
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
219580-11-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

Background References

  1. Activation of glial FGFRs is essential in glial migration, proliferation, and survival and in glia-neuron signaling during olfactory system development.
    Gibson NJ, Tolbert LP, Oland LA
    PLoS ONE, 2012;7(4):e33828.
  2. Step-Wise Chondrogenesis of Human Induced Pluripotent Stem Cells and Purification Via a Reporter Allele Generated by CRISPR-Cas9 Genome Editing
    SS Adkar, CL Wu, VP Willard, A Dicks, A Ettyreddy, N Steward, N Bhutani, CA Gersbach, F Guilak
    Stem Cells, 2018;0(0):.
  3. A Molecular atlas of Xenopus respiratory system development.
    Rankin S, Thi Tran H, Wlizla M, Mancini P, Shifley E, Bloor S, Han L, Vleminckx K, Wert S, Zorn A
    Dev Dyn, 2015;244(1):69-85.
  4. Increased FGF1-FGFRc expression in idiopathic pulmonary fibrosis.
    MacKenzie B, Korfei M, Henneke I, Sibinska Z, Tian X, Hezel S, Dilai S, Wasnick R, Schneider B, Wilhelm J, El Agha E, Klepetko W, Seeger W, Schermuly R, Gunther A, Bellusci S
    Respir Res, 2015;16(0):83.
  5. Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors.
    Wilson TR, Fridlyand J, Yan Y, Penuel E, Burton L, Chan E, Peng J, Lin E, Wang Y, Sosman J, Ribas A, Li J, Moffat J, Sutherlin DP, Koeppen H, Merchant M, Neve R, Settleman J
    Nature, 2012;487(7408):505-9.
  6. FGF8 and SHH substitute for anterior-posterior tissue interactions to induce limb regeneration

    Nature, 2016;533(7603):407-10.
  7. The role of HGF/MET and FGF/FGFR in fibroblast-derived growth stimulation and lapatinib-resistance of esophageal squamous cell carcinoma.
    Saito S, Morishima K, Ui T, Hoshino H, Matsubara D, Ishikawa S, Aburatani H, Fukayama M, Hosoya Y, Sata N, Lefor A, Yasuda Y, Niki T
    BMC Cancer, 2015;15(0):82.
  8. Oncogenic mutations in intestinal adenomas regulate Bim-mediated apoptosis induced by TGF-beta.
    Wiener Z, Band A, Kallio P, Hogstrom J, Hyvonen V, Kaijalainen S, Ritvos O, Haglund C, Kruuna O, Robine S, Louvard D, Ben-Neriah Y, Alitalo K
    Proc Natl Acad Sci U S A, 2014;111(21):E2229-36.
  9. Specific inhibitor of FGF receptor signaling: FGF-2-mediated effects on proliferation, differentiation, and MAPK activation are inhibited by PD173074 in oligodendrocyte-lineage cells.
    Bansal et al.
    J.Neurosci.Res., 2003;74:486
  10. Conversion of mouse epiblast stem cells to an earlier pluripotency state by small molecules.
    Zhou et al.
    J.Biol.Chem., 2010;285:29676
  11. Capture of authentic embryonic stem cells from rat blastocysts.
    Buehr et al.
    Cell, 2008;135:1287
  12. The Axonal Membrane Protein PRG2 Inhibits PTEN and Directs Growth to Branches
    A Brosig, J Fuchs, F Ipek, C Kroon, S Schrötter, M Vadhvani, A Polyzou, J Ledderose, M van Diepen, HG Holzhütter, T Trimbuch, N Gimber, J Schmoranze, I Lieberam, C Rosenmund, C Spahn, P Scheerer, M Szczepek, G Leondariti, BJ Eickholt
    Cell Rep, 2019;29(7):2028-2040.e8.
  13. 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 bla
    Miyake et al.
    J.Pharmacol.Exp.Ther., 2010;332:795

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Citations for PD 173074

The citations listed below are publications that use Tocris products. Selected citations for PD 173074 include:

20 Citations: Showing 1 - 10

  1. Ciliary neurotrophic factor stimulates cardioprotection and the proliferative activity in the adult zebrafish heart.
    Authors: Bise Et al.
    NPJ Regen Med  2019;4:2
  2. IFT80 is required for stem cell proliferation, differentiation, and odontoblast polarization during tooth development.
    Authors: Yuan Et al.
    Cell Death Dis  2019;10:63
  3. Self-patterning of rostral-caudal neuroectoderm requires dual role of Fgf signaling for localized Wnt antagonism.
    Authors: Takata Et al.
    Nat Commun  2017;8:1339
  4. Epidermal β-catenin activation remodels the dermis via paracrine signalling to distinct fibroblast lineages.
    Authors: Lichtenberger Et al.
    Nat Commun  2016;7:10537
  5. FGF8 and SHH substitute for anterior-posterior tissue interactions to induce limb regeneration.
    Authors: Nacu Et al.
    Nature  2016;533:407
  6. A kinome-targeted RNAi-based screen links FGF signaling to H2AX phosphorylation in response to radiation.
    Authors: Benzina Et al.
    Stem Cells Int  2015;72:3559
  7. Fibroblast surface-associated FGF-2 promotes contact-dependent colorectal cancer cell migration and invasion through FGFR-SRC signaling and integrin αvβ5-mediated adhesion.
    Authors: Knuchel Et al.
    Development  2015;6:14300
  8. A Molecular atlas of Xenopus respiratory system development.
    Authors: Rankin Et al.
    PLoS One  2015;244:69
  9. Inhibition of G9a Histone Methyltransferase Converts Bone Marrow Mesenchymal Stem Cells to Cardiac Competent Progenitors.
    Authors: Yang Et al.
    Dev Dyn  2015;2015:270428
  10. Increased FGF1-FGFRc expression in idiopathic pulmonary fibrosis.
    Authors: MacKenzie Et al.
    Respir Res  2015;16:83
  11. The role of HGF/MET and FGF/FGFR in fibroblast-derived growth stimulation and lapatinib-resistance of esophageal squamous cell carcinoma.
    Authors: Saito Et al.
    BMC Cancer  2015;15:82
  12. PD173074, a selective FGFR inhibitor, reverses MRP7 (ABCC10)-mediated MDR.
    Authors: Anreddy Et al.
    Development  2014;4:202
  13. Generation of the epicardial lineage from human pluripotent stem cells.
    Authors: Witty Et al.
    Nat Biotechnol  2014;32:1026
  14. Modulation of pluripotency in the porcine embryo and iPS cells.
    Authors: Rodríguez Et al.
    Acta Pharm Sin B  2012;7:e49079
  15. Activation of glial FGFRs is essential in glial migration, proliferation, and survival and in glia-neuron signaling during olfactory system development.
    Authors: Gibson Et al.
    PLoS One  2012;7:e33828
  16. Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors.
    Authors: Wilson Et al.
    Nature  2012;487:505
  17. The existence of FGFR1-5-HT1A receptor heterocomplexes in midbrain 5-HT neurons of the rat: relevance for neuroplasticity.
    Authors: Borroto-Escuela Et al.
    J Neurosci  2012;32:6295
  18. Suppression of Bmp4 signaling by the zinc-finger repressors Osr1 and Osr2 is required for Wnt/β-catenin-mediated lung specification in Xenopus.
    Authors: Rankin Et al.
    Cell Mol Life Sci  2012;139:3010
  19. Conversion from mouse embryonic to extra-embryonic endoderm stem cells reveals distinct differentiation capacities of pluripotent stem cell states.
    Authors: Cho Et al.
    J Biol Chem  2012;139:2866
  20. Prolonged FGF signaling is necessary for lung and liver induction in Xenopus.
    Authors: Shifley Et al.
    BMC Dev Biol  2012;12:27

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