Linsitinib - CAS 867160-71-2
Catalog number: 867160-71-2
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
IGF-1R
Description:
Linsitinib, also known as OSI-906, is  an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity.  OSI-906 selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGFR-1 stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.
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Appearance:
white solid powder
Synonyms:
OSI-906; OSI906; OSI 906.
MSDS:
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Current Developer:
OSI Pharmaceuticals, Inc.
1.Phase I Dose-Escalation Study of Linsitinib (OSI-906) and Erlotinib in Patients with Advanced Solid Tumors.
Macaulay VM1, Middleton MR2, Eckhardt SG3, Rudin CM4, Juergens RA5, Gedrich R6, Gogov S7, McCarthy S8, Poondru S9, Stephens AW10, Gadgeel SM11. Clin Cancer Res. 2016 Feb 1. [Epub ahead of print]
PURPOSE: Cross-talk between type I IGF receptor (IGF1R), insulin receptor (INSR), and epidermal growth factor receptor (EGFR) mediates resistance to individual receptor blockade. This study aimed to determine the MTD, safety, pharmacokinetics, pharmacodynamics, and preliminary antitumor activity of linsitinib, a potent oral IGF1R/INSR inhibitor, with EGFR inhibitor erlotinib.
2.Mass balance, pharmacokinetics, and metabolism of linsitinib in cancer patients.
Poondru S1, Chaves J2, Yuen G3, Parker B4, Conklin E5, Singh M3, Nagata M5, Gill S3. Cancer Chemother Pharmacol. 2016 Apr;77(4):829-37. doi: 10.1007/s00280-016-2999-5. Epub 2016 Mar 14.
PURPOSE: This study characterized the pharmacokinetics, mass balance, routes and extent of elimination, metabolites, and safety of a single oral dose of (14)C-linsitinib, an IGF-1R/IR inhibitor, in patients with advanced solid tumors. The tolerability of linsitinib after multiple-dose administration was assessed in those patients who wished to continue treatment beyond the single (14)C-linsitinib dose.
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CAS 867160-71-2 Linsitinib

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