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OSI-906 (Linsitinib) | IFG-1R/IR inhibitor

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Price:
$169.00
Catalog #:
C6906-5
Quantity:


Product Description

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.

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