In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase.

@article{Panek1998InVB,
  title={In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase.},
  author={Robert L. Panek and Gina H Lu and Tawny Dahring and B. L. Batley and Caitlin Connolly and James M Hamby and Kathryn J. Brown},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1998},
  volume={286 1},
  pages={569-77}
}
Through direct synthetic efforts, we discovered a small molecule that is a nanomolar inhibitor of the human fibroblast growth factor-1 receptor (FGFR) tyrosine kinase. PD 166866, a member of a new structural class of tyrosine kinase inhibitors, the 6-aryl-pyrido[2,3-d]pyrimidines, was identified by screening a compound library with assays that measure protein tyrosine kinase activity. PD 166866 inhibited human full-length FGFR-1 tyrosine kinase with an IC50 value of 52.4 +/- 0.1 nM and was… CONTINUE READING

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References

Publications referenced by this paper.
Showing 1-10 of 34 references

Pyrido[2,3-D]pyrimidines for inhibiting protein tyrosine kinase mediated cellular proliferation

CJ Blankley, DH Boschelli, +3 authors RL Panek
1997
View 4 Excerpts
Highly Influenced

GraFit User’s Guide, Version 3.0

RJ Leatherbarrow
Erithacus Software Ltd., • 1992
View 2 Excerpts
Highly Influenced

A novel in vitro assay for human angiogenesis.

Laboratory investigation; a journal of technical methods and pathology • 1996
View 8 Excerpts

Phenylamino-pyrimidine (PAP)-derivatives: A new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors

J Zimmermann, E Buchdunger, +3 authors P Traxler
Bioorg Med Chem Lett 6:1221–1226 • 1996
View 2 Excerpts

A synthetic inhibitor of the mitogen-activated protein kinase cascade.

Proceedings of the National Academy of Sciences of the United States of America • 1995
View 2 Excerpts

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