PD 166285

PD 166285 is a tyrosine kinase inhibitor.¹ It inhibits Src, FGFR1, EGFR, and PDGFRβ (IC₅₀s = 8.4, 39.3, 87.5, and 98.3 nM, respectively), as well as WEE1 (IC₅₀ = 24 nM).^1,2 PD 166285 inhibits PDGF- or EGF-induced receptor autophosphorylation in vascular smooth muscle cells (VSMCs) and A431 cells, respectively, and bFGF-induced tyrosine phosphorylation in Sf9 cells (IC₅₀s = 6.5, 1,600, and 97.3 nM, respectively).¹ It also inhibits chemotaxis and growth of, as well as adhesion to vitronectin by, VSMCs (IC₅₀s = 80-120 nM). PD 166285 inhibits radiation-induced cell cycle arrest at the G₂/M phase and enhances radiation-induced cell death in HT-29 cells.² In vivo, PD 166285 (1, 5, and 10 mg/kg) inhibits angiogenesis and induces tumor regression in a 16c murine mammary carcinoma model when administered in combination with photodynamic therapy (PDT).³

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1. Panek, R.L., Lu, G.H., Klutchko, S.R., et al. In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor. J. Pharmacol. Exp. Ther. 283(3), 1433-1444 (1997).

2. Wang, Y., Li, J., Booher, R.N., et al. Radiosensitization of p53 mutant cells by PD0166285, a novel G₂ checkpoint abrogator. Cancer Res. 61(22), 8211-8217 (2001).

3. Dimitroff, C.J., Klohs, W., Sharma, A., et al. Anti-angiogenic activity of selected receptor tyrosine kinase inhibitors, PD166285 and PD173074: Implications for combination treatment with photodynamic therapy. Invest. New Drugs 17(2), 121-135 (1999).