Potent inhibitor of the tyrosine kinases c-Src, fibroblast growth factor receptor 1 (FGFR1), and platelet-derived growth factor receptor β (PDGFRβ) (IC50 values are 8.4, 39.3 and 98.3 nM respectively). Also inhibits the checkpoint kinases Wee1 and Myt1; abolishes Cdc2 phosphorylation in numerous tumor cell lines and abrogates the G2 checkpoint.
Panek et al (1997) In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor. J.Pharmacol.Exp.Ther. 283 1433 PMID:9400019 |Wang et al (2001) Radiosensitization of p53 mutant cells by PD0166285, a novel G2 checkpoint abrogator. Cancer Res. 61 8211 PMID:11719452 |Hashimoto et al (2006) Cell cycle regulation by the Wee1 inhibitor PD0166285, Pyrido [2,3-d] pyimidine, in the B16 mouse melanoma cell line. BMC Cancer 6 292 PMID:17177986