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PD 173074

Cat No. 3044

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

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

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 and MSDS.

Resources

Certificate of Analysis / MSDS

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Material Safety Data Sheet: View current batch

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References

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