Linsitinib ≥98%

Potent and selective dual IGF-1R (IC₅₀ = 35 nM in cell-free assay) and Insulin Receptor (IC₅₀ = 75 nM in cell-free assay) kinase inhibitor. Inactive towards Abl, ALK, BTK, EGFR, FGFR1/2 and PKA. Displayed <50% inhibition at 1 μM against a panel of 88 kinases. Blocks IGF-1R autophosphorylation and downstream activation of Akt, ERK1/2 and S6 kinase. Blocks tumor cell line proliferation. Blocks IGF-1R driven tumor xenograft growth.

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