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.

≥99%

Soluble in DMSO at 100 mg/ml; soluble in ethanol at 200 mg/ml; very poorly soluble in water; maximum solubility in plain water is estimated to be about 50-100 µM.

Crystalline solid.

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

Mohammadi, M., et al.  EMBO J. 17:  5896-5904 (1998).

Kinase

Inhibitor