OSI-906 (Linsitinib) is an orally-available, ATP-competitive, imidazopyrazine-based dual inhibitor of IGF-R1 and IR with IC50 biochemical potency of 35 nM and 75 nM, respectively. [1] In vitro cell assays reveal that OSI-906 potently inhibits IGF-1R, pERK1/2, and p-70S6K at IC50s of 24, 28, and 60 nM, respectively. In HT-29 and Colo205 CRC cells, oSI-906 fully inhibits both IR and IGF-1R phosphorylation, with antiproliferative effects at EC50 of 210 nM and 320 nM, respectively.
Oral, in vivo efficacy studies (QDx12) of OSI-906 in a LISN xenograft model resulted in a dose-dependent effect on tumor growth inhibition with 100% TGI and 55% regression at 75 mg/kg, and 60% TGI at 25 mg/kg.
Technical information:
| Chemical Formula: | C26H23N5O | |
| CAS #: | 867160-71-2 | |
| Molecular Weight: | 421.49 | |
| Purity: | >98% | |
| Appearance: | Yellow | |
| Chemical Name: | (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | OSI-906, OSI 906, OSI906, Linsitinib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Mulvihill et al., Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med. Chem. 2009, 1(6), 1153-1171. Pubmed ID: 21425998 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
