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OSI-906

Cat. No. M1821
OSI-906 Structure
Synonym:

Linsitinib

Size Price Availability Quantity
10mg USD 210 In stock
50mg USD 500 In stock
100mg USD 850 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

OSI-906 (Linsitinib) is an orally small-molecule inhibitor of IGF-1R with potential antineoplastic activity. IGF-1R has been viewed as an important therapeutic target due to its involvement in the growth and proliferation in a variety of human cancers, including adrenocortical carcinoma (ACC), ovarian and non-small cell lung cancers. A major challenge in the development of IGF-1R inhibitors is to avoid blocking the closely related insulin receptor that regulates glucose levels in the blood. OSI-906 (Linsitinib) 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. OSI-906 slowed the growth of IGF-1R-dependent tumors, and it also reduced proliferation and/or survival of a broad panel of tumor cell lines.

Protocol
Cell Experiment
Cell lines NSCLC(H292, H358 and H1703) and CRC(Colo205, HT-29 and RKO) tumor cell lines
Preparation method Cell proliferation assay. cells were seeded into 96-well plates in appropriate media containing FCS 10% and incubated for 3 days in the presence of OSI-906 at various concentrations. Inhibition of cell growth was determined by luminescent quantitation of intracellular ATP content using CellTiterGlo (Promega, Madision , WI, USA). Data were presented as a fraction of maximal proliferation, caculated by dividing the cellular density in the presence of varying concentrations of OSI-906 by the cellular density of control cells treated with vehicle (DMSO) only.
Concentrations 0~10 μM
Incubation time 72 h
Animal Experiment
Animal models LISN tumor xenograft model in mice
Formulation 25mM tartaric acid
Dosages 25mg/kg or 75mg/kg daily for 12 days
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 421.49
Formula C26H23N5O
CAS Number 867160-71-2
Purity >99%
Solubility DMSO ≥84 mg/mL
Storage at -20°C
References

Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor.
Mulvihill MJ, et al. Future Med Chem. 2009 Sep;1(6):1153-71. PMID: 21425998.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: OSI-906, Linsitinib supplier, IGF-1R, inhibitors

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