Cayman GSK1838705A

GSK1838705A is an inhibitor of the insulin-like growth factor-1 receptor (IGF-1R) and the insulin receptor (IR; IC₅₀s = 2 and 1.6 nM, respectively).¹ It is selective for IGF-1R and IR over a panel of 47 kinases (IC₅₀s = >1,600 nM), however, it also inhibits anaplastic lymphoma kinase (ALK; IC₅₀ = 0.5 nM). GSK1838705A inhibits IGF-1 and insulin-induced phosphorylation of IGF-1R and IR in a concentration-dependent manner as well as phosphorylation of the downstream signaling markers Akt, IRS-1, and ERK in MCF-7 breast carcinoma cells. It inhibits growth in a panel of cancer cell lines (EC₅₀s = 24-8,378 nM) with the IGF-1R signaling-dependent multiple myeloma and Ewings sarcoma cell lines being the most sensitive. In vivo, GSK1838705A completely inhibits IGF-1-induced phosphorylation of IGF-1R, Akt, and IRS-1 as well as reduces tumor growth in the COLO 205 and NIH-3T2/LISN mouse xenograft models when administered at doses of ≥1 and ≥10 mg/kg, respectively. It also induces tumor cell apoptosis and reduces tumor growth in U87MG glioma and PC3R prostate cancer mouse xenograft models.^2,3

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