• PD 173074 selectively inhibits the tyrosine kinase activities of the FGF and VEGF receptors.
• PD 173074 inhibited the kinase activity of FGFR1 with an IC50 of 25 nM in vitro, while inhibiting Src, the receptors for insulin, epidermal growth factor (EGF) and PDGF, and several serine/threonine kinases with 1000-fold or higher IC50 values. PD 173074 was an ATP-competitive inhibitor of FGFR1, with a Ki of around 40 nM. PD 173074 inhibited autophosphorylation of FGFR1 and VEGFR2 in a dose-dependent manner with IC50s in the range of 1-5 nM and 100-200 nM, respectively. Mice treated daily with PD 173074 exhibited dose-dependent inhibition of FGF-induced and VEGF-induced neovascularization. However, PD 173074 was somewhat less effective in blocking VEGF-induced than FGF-induced angiogenesis. Mohammadi, M., et al. "Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain." EMBO J. 17: 5896-5904 (1998).
• PD 173074 inhibited cell proliferation of two low-grade, noninvasive human bladder urothelial carcinoma (UC) cell lines, UM-UC-14 and MGHU3, which expressed mutated FGFR3 protein. However, the other six cell lines expressing wild-type FGFR3 or without FGFR3 expression were resistant to PD 173074 treatment. In the mouse xenograft models subcutaneously transplanted with these two cell lines, orally administered PD173074 suppressed tumor growth and induced apoptosis. Miyake, M., et al. "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: 795-802 (2010).
• The FGFR1 inhibitor PD 173074 dose-dependently inhibited FGF-2 promotion of granule neuron survival under low-potassium, serum-free conditions with IC50 of 12 nM, when added together with FGF-2 for a 24-h pretreatment prior to potassium withdrawal. Skaper, S.D., et al. "The FGFR1 inhibitor PD 173074 selectively and potently antagonizes FGF-2 neurotrophic and neurotropic effects." J. Neurochem. 75: 1520-1527 (2000).
• PD 173074 inhibited the proliferation and clonogenic growth of small cell lung cancer cell lines H-510 and H-69 in vitro and in vivo. It also prevented FGF-2-induced chemoresistance. These effects correlated with the inhibition of both FGFR1 and FGFR2 transphosphorylation. Pardo, O.E., et al. "The fibroblast growth factor receptor inhibitor PD173074 blocks small cell lung cancer growth in vitro and in vivo." Cancer Res. 69: 8645-8651 (2009).
• PD 173074 inhibited the growth of glioblastoma cells in vitro. Loilome, W., et al. "Glioblastoma cell growth is suppressed by disruption of Fibroblast Growth Factor pathway signaling." J. Neurooncol. 94: 359-366 (2009).
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
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