Linsitinib

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    WARNING: This product is for research use only, not for human or veterinary use.

Description: Linsitinib, also known as OSI-906, is a n 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.

Price and Availability

Linsitinib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Synonym: OSI906; OSI-906; OSI 906; Linsitinib.

IUPAC/Chemical Name: (1r,3r)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol.

InChi Key: PKCDDUHJAFVJJB-KQODVJPSSA-N

InChi Code: InChI=1S/C26H23N5O/c1-26(32)14-19(15-26)25-30-22(23-24(27)28-11-12-31(23)25)18-8-7-17-9-10-20(29-21(17)13-18)16-5-3-2-4-6-16/h2-13,19,32H,14-15H2,1H3,(H2,27,28)/t19-,26-

SMILES Code: O[C@@]1(C)C[C@H](C2=NC(C3=CC=C4C=CC(C5=CC=CC=C5)=NC4=C3)=C6C(N)=NC=CN62)C1

Technical Data

References

1: Zhang H, Kathawala RJ, Wang YJ, Zhang YK, Patel A, Shukla S, Robey RW, Talele TT, Ashby CR Jr, Ambudkar SV, Bates SE, Fu LW, Chen ZS. Linsitinib (OSI-906) antagonizes ATP-binding cassette subfamily G member 2 and subfamily C member 10-mediated drug resistance. Int J Biochem Cell Biol. 2014 Jun;51:111-9. doi: 10.1016/j.biocel.2014.03.026. Epub 2014 Apr 12. PubMed PMID: 24726739.

2: Shirakawa J, Okuyama T, Yoshida E, Shimizu M, Horigome Y, Tuno T, Hayasaka M, Abe S, Fuse M, Togashi Y, Terauchi Y. Effects of the antitumor drug OSI-906, a dual inhibitor of IGF-1 receptor and insulin receptor, on the glycemic control, β-cell functions, and β-cell proliferation in male mice. Endocrinology. 2014 Jun;155(6):2102-11. doi: 10.1210/en.2013-2032. Epub 2014 Apr 8. PubMed PMID: 24712877.

3: Leiphrakpam PD, Agarwal E, Mathiesen M, Haferbier KL, Brattain MG, Chowdhury S. In vivo analysis of insulin-like growth factor type 1 receptor humanized monoclonal antibody MK-0646 and small molecule kinase inhibitor OSI-906 in colorectal cancer. Oncol Rep. 2014 Jan;31(1):87-94. doi: 10.3892/or.2013.2819. Epub 2013 Oct 25. PubMed PMID: 24173770; PubMed Central PMCID: PMC3868504.

4: Zhao H, Desai V, Wang J, Epstein DM, Miglarese M, Buck E. Epithelial-mesenchymal transition predicts sensitivity to the dual IGF-1R/IR inhibitor OSI-906 in hepatocellular carcinoma cell lines. Mol Cancer Ther. 2012 Feb;11(2):503-13. doi: 10.1158/1535-7163.MCT-11-0327. Epub 2011 Dec 9. PubMed PMID: 22161861.

5: McKinley ET, Bugaj JE, Zhao P, Guleryuz S, Mantis C, Gokhale PC, Wild R, Manning HC. 18FDG-PET predicts pharmacodynamic response to OSI-906, a dual IGF-1R/IR inhibitor, in preclinical mouse models of lung cancer. Clin Cancer Res. 2011 May 15;17(10):3332-40. doi: 10.1158/1078-0432.CCR-10-2274. Epub 2011 Jan 21. PubMed PMID: 21257723; PubMed Central PMCID: PMC3122480.

6: Mulvihill MJ, Cooke A, Rosenfeld-Franklin M, Buck E, Foreman K, Landfair D, O'Connor M, Pirritt C, Sun Y, Yao Y, Arnold LD, Gibson NW, Ji QS. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med Chem. 2009 Sep;1(6):1153-71. doi: 10.4155/fmc.09.89. PubMed PMID: 21425998.