PD 173074

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Cat.No. 3044 - PD 173074 | C28H41N7O3 | CAS No. 219580-11-7
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% (HPLC)
Datasheet
Citations (17)
Reviews
Literature

Biological Activity

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. Suppresses cell proliferation in cell lines expressing mutated FGFR3 protein. Blocks tumor growth in H510 and H69 SCLC xenograft models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries

PD 173074 is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 523.67
Formula C28H41N7O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 219580-11-7
PubChem ID 1401
InChI Key DXCUKNQANPLTEJ-UHFFFAOYSA-N
Smiles O=C(NC(C)(C)C)NC2=NC1=NC(NCCCCN(CC)CC)=NC=C1C=C2C3=CC(OC)=CC(OC)=C3

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 52.37 100
ethanol 52.37 100

Preparing Stock Solutions

The following data is based on the product molecular weight 523.67. Batch specific molecular weights may vary from batch to batch due to solvent 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 1.91 mL 9.55 mL 19.1 mL
5 mM 0.38 mL 1.91 mL 3.82 mL
10 mM 0.19 mL 0.95 mL 1.91 mL
50 mM 0.04 mL 0.19 mL 0.38 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

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

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 bla J.Pharmacol.Exp.Ther. 332 795 PMID: 19955487

Trudel et al (2004) Inhibition of fibroblast growth factor receptor 3 induces differentiation and apoptosis in t(4;14) myeloma. Neoplasia 103 3521

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


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Keywords: PD 173074, PD 173074 supplier, Selective, FGFR1, FGFR3, inhibitors, inhibits, fibroblast, growth, factors, PD173074, stem, cells, Pfizer, FGFR, Stem, Cell, Proliferation, Neural, Cells, 3044, Tocris Bioscience

17 Citations for PD 173074

Citations are publications that use Tocris products. Selected citations for PD 173074 include:

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

Benzina et al (2015) A kinome-targeted RNAi-based screen links FGF signaling to H2AX phosphorylation in response to radiation. Stem Cells Int 72 3559 PMID: 25894690

Yang et al (2015) Inhibition of G9a Histone Methyltransferase Converts Bone Marrow Mesenchymal Stem Cells to Cardiac Competent Progenitors. Dev Dyn 2015 270428 PMID: 26089912

Rankin et al (2015) A Molecular atlas of Xenopus respiratory system development. PLoS One 244 69 PMID: 25156440

Knuchel et al (2015) Fibroblast surface-associated FGF-2 promotes contact-dependent colorectal cancer cell migration and invasion through FGFR-SRC signaling and integrin αvβ5-mediated adhesion. Development 6 14300 PMID: 25973543

Witty et al (2014) Generation of the epicardial lineage from human pluripotent stem cells. Nat Biotechnol 32 1026 PMID: 25240927

Rankin et al (2012) Suppression of Bmp4 signaling by the zinc-finger repressors Osr1 and Osr2 is required for Wnt/β-catenin-mediated lung specification in Xenopus. Cell Mol Life Sci 139 3010 PMID: 22791896

Cho et al (2012) Conversion from mouse embryonic to extra-embryonic endoderm stem cells reveals distinct differentiation capacities of pluripotent stem cell states. J Biol Chem 139 2866 PMID: 22791892

Rodríguez et al (2012) Modulation of pluripotency in the porcine embryo and iPS cells. Acta Pharm Sin B 7 e49079 PMID: 23145076

Lichtenberger et al (2016) Epidermal β-catenin activation remodels the dermis via paracrine signalling to distinct fibroblast lineages. Nat Commun 7 10537 PMID: 26837596

Nacu et al (2016) FGF8 and SHH substitute for anterior-posterior tissue interactions to induce limb regeneration. Nature 533 407 PMID: 27120163

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

Wilson et al (2012) Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors. Nature 487 505 PMID: 22763448

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

Shifley et al (2012) Prolonged FGF signaling is necessary for lung and liver induction in Xenopus. BMC Dev Biol 12 27 PMID: 22988910

MacKenzie et al (2015) Increased FGF1-FGFRc expression in idiopathic pulmonary fibrosis. Respir Res 16 83 PMID: 26138239

Anreddy et al (2014) PD173074, a selective FGFR inhibitor, reverses MRP7 (ABCC10)-mediated MDR. Development 4 202 PMID: 26579384


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