Linsitinib
IGF-1R kinase / InsR kinase inhibitor / Linsitinib is a potent and selective dual inhibitor of insulin-like growth factor 1 (IGF-1R) kinase and insulin receptor (InsR) kinase (IC50’s = 35 and 75 nM respectively).1 It has been investigated as a chemotherapeutic in combination with other drugs for various cancers.2-6
Biochemicals & reagents
867160-71-2
OSI-906
1) Mulvihill et al. (2009), Discovery of OSI-906: a selective and orally efficacious inhibitor of the IGF-1 receptor and insulin receptor; Future Med.Chem. 1 1153 2) Bendell et al. (2015), A phase Ib study of linsitinib (OSI-906), a dual inhibitor of IGF-1R and IR tyrosine kinase, in combination with everolimus as treatment for patients with refractory metastatic colorectal cancer; Invest.New Drugs 33 187 3) Pivonello et al. (2016), The dual targeting of insulin and insulin-like growth factor 1 receptor enhances the mTOR inhibitor-mediated antitumor efficacy in hepatocellular carcinoma ; Oncotarget 7 9718 4) Lee et al. (2016), Inhibition of IGF1R signaling abrogates resistance to afatinib (BIBW2992) in EGFR T790M mutant lung cancer cells; Mol.Carcinog. 55 991 5) Macaulay et al. (2016), Phase I Dose-Escalation Study of Linsitinib (OSI-906) and Erlotinib in Patients with Advanced Solid Tumors; Clin.Cancer Res. 22 2897 6) De Lint et al. (2016), Sensitizing Triple-Negative Breast Cancer to PI3K Inhibition by Cotargeting IGF1R; Mol.Cancer Ther. 15 1545
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TARGET: Kinase -- DISEASE AREA: Cancer