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Cat. No. Name Size Price Add Cart
KI0172Osi-9065 mg$272
Osi-90610 mg$432
Osi-90650 mg$1152
Osi-906200 mg$2672

Chemical Characteristic

Product NameOsi-906
SynonymsLinsitinib
CAS No.867160-71-2
Molecular Weight 421.49
FormulaC26H23N5O
Chemical Name(1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol
Smiles[C@]1(C[C@H](C1)c1n2c(c(ncc2)N)c(n1)c1ccc2ccc(nc2c1)c1ccccc1)(O)C
Chemical Structure

Biological activities

Osi-906 is a selective and orally efficacious dual inhibitor of the IGF-1 (insulin-like growth factor 1) receptor and insulin receptor (IR). The IC50 of osi-906 is 35 and 75 nM against IGF-IR and IR, respectively. Osi-906 inhibits IGF-1R-CHO cell line with an IC50 of 5 nM.[1] In cell-based phenotypic assays, osi-906 inhibits IGF-1- or IGF-2-mediated proliferation.[2] Osi-906 potently and selectively inhibits autophosphorylation of both human IGF-1R and IR. Osi-906 displays in vitro antiproliferative effects in a variety of tumor cell lines including Colo205, HT-29 and RKO cells. Osi-906 fully blocks IGF-1-stimulated receptor phosphorylation in the LISN cells.[3] Osi-906 demonstrates significant TGI (tumor growth inhibition) effects in multiple tumor xenograft models, including NIH-3T3/LISN, GEO, H295, and IGF-1R and IR DC models.[1] Uptake of 3H-2-deoxy glucose and 18FDG is significantly diminished following osi-906 exposure in sensitive tumor cells and subcutaneous xenografts (NCIH292) but not in an insensitive model lacking IGF-1R expression (NCI-H441).[4] Osi-906 in combination with bortezomib overcome bortezomib resistance in an in vivo model of myeloma.[5]

References

[1] Jin M, et al. Small-molecule ATP-competitive dual IGF-1R and insulin receptor inhibitors: structural insights, chemical diversity and molecular evolution. Future Med Chem. 2012, 4(3): 315-328.
[2] Mulvihill MJ, 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.
[3] Mulvihill MJ, 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.
[4] McKinley ET, et al. 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, 17(10): 3332-3340.
[5] Kuhn DJ, et al. Targeting the insulin-like growth factor-1 receptor to overcome bortezomib resistance in pre-clinical models of multiple myeloma. Blood. 2012

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