Cayman C25-140

PKI-166 is an ATP-competitive inhibitor of the EGF receptor (EGFR; IC₅₀ = 0.0007 µM for the intracellular kinase domain). It is selective for the EGFR intracellular kinase domain over the serine/threonine kinases PKCα and Cdc2/cyclin B (IC₅₀s = >100 and 78 µM, respectively), as well as FLK, c-Met, and Tek (IC₅₀ = >1 µM for all), but does inhibit c-Src, c-Abl, VEGFR2/KDR, FLT1, and c-Kit (IC₅₀s = 0.103, 0.028, 0.327, 0.962, and 2.21 µM, respectively). PKI-166 prevents phosphorylation of EGFR induced by EGF in L3.6pl pancreatic cancer cells in a concentration-dependent manner. It enhances the cytotoxicity of gemcitabine (Item No. ) in L3.6pl cells and reduces tumor growth and metastasis and increases survival in an L3.6pl mouse xenograft model when administered alone at a dose of 100 mg/kg per day with additive effects on these parameters when administered in combination with gemcitabine. PKI-166 also reduces tumor growth and inhibits angiogenesis in an SN12-PM6 human renal cell carcinoma mouse orthotopic model.

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