BM001 (BM-001) is a small molecular inhibitor of the integral growth hormone/insulin-like growth factor-1 (GH/IGF1) axis, shows potent antiproliferative effect on cancer cells MDA-MM-231 and Colo-205 with IC50 of 20-30 nM.
AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.
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