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Tocris/PD 173074/3044/10/10 mg

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货号: 3044/10

品牌: Tocris

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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% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

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 PMID:

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 PMID:

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

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