AZ12253801 is an ATP-competitive inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), demonstrating approximately 10-fold selectivity over the insulin receptor. It exhibits potent inhibition of IGF-1R-mediated proliferation in 3T3 mouse fibroblasts transfected with human IGF-1R, with an IC50 value of 17 nmol/L. Additionally, AZ12253801 shows reduced activity against epidermal growth factor receptor (EGFR)-driven proliferation, with an IC50 of 440 nmol/L. Its characteristics make it a valuable tool for investigating anti-tumor mechanisms and IGF-1R signaling pathways in cancer research.
AZ12253801 is an ATP-competitive inhibitor of the insulin-like growth factor 1 receptor (IGF-1R), demonstrating approximately 10-fold selectivity over the insulin receptor. It exhibits potent inhibition of IGF-1R-mediated proliferation in 3T3 mouse fibroblasts transfected with human IGF-1R, with an IC50 value of 17 nmol/L. Additionally, AZ12253801 shows reduced activity against epidermal growth factor receptor (EGFR)-driven proliferation, with an IC50 of 440 nmol/L. Its characteristics make it a valuable tool for investigating anti-tumor mechanisms and IGF-1R signaling pathways in cancer research.
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