FGFR/VEGFR Tyrosine Kinase Inhibitor

No.177(April 2018)

P2474: PD173074 (1)

PD173074 (1) inhibits the tyrosine kinase activities of the fibroblast growth factor receptor (FGFR) and vascular endothelial growth factor receptor (VEGFR) (Table 1).¹⁾ The inhibitory manner of 1 is ATP-competitive and the inhibitory constants (Ki) of 1 to FGFR1 and its cytoplasmic domain are 45.2±4.8 nM and 36.4±3.6 nM, respectively.

1 also inhibits the differentiation of mouse and human embryo stem cells^2,3) and human induced pluripotent stem cells.⁴⁾

Table 1. Inhibitory activity of PD173074

This product is for research purpose only.

References

1)Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain
- M. Mohammadi, S. Froum, J. H. Hamby, M. C. Schroeder, R. L. Panek, G. H. Lu, A. V. Eliseenkova, D. Green, J. Schlessinger, S. R. Hubbard, EMBO J. 1998, 17, 5896.
2)The ground state of embryonic stem cell self-renewal
- Q.-L. Ying, J. Wray, J. Nichols, L. Batlle-Morera, B. Doble, J. Woodgett, P. Cohen, A. Smith, Nature 2008, 453, 519.
3)Human embryonic stem cells with biological and epigenetic characteristics similar to those of mouse ESCs
- J. Hanna, A. W. Cheng, K. Saha, J. Kim, C. J. Lengner, F. Soldner, J. P. Cassady, J. Muffat, B. W. Carey, R. Jaenisch, Proc. Natl. Acad. Sci. USA 2010, 107, 9222.
4)Virus-free induction of pluripotency and subsequent excision of reprogramming factors
- K. Kaji, K. Norrby, A. Paca, M. Mileikovsky, P. Mohseni, K. Woltjen, Nature 2009, 458, 771.

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FGFR/VEGFR Tyrosine Kinase Inhibitor

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