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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.
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Source | Oncol Rep (2014). Figure 3. OSI-906 |
| Method | TUNEL assay | |
| Cell Lines | GEO cells | |
| Concentrations | 50~1000 nM | |
| Incubation Time | 48 h | |
| Results | Both MK-0646 and OSI-906 treated GEO xenografts had statistically significant increase in apoptosis (p<0.05) as compared with the control tumors |
| 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 |
| Molecular Weight | 421.49 |
| Formula | C26H23N5O |
| CAS Number | 867160-71-2 |
| Solubility (25°C) | DMSO 62 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| IGF-I (24-41)
IGF-I (24-41) (Insulin-like Growth Factor I (24-41)) is amino acids 24 to 41 fragment of IGF-I. |
| GIP, human
GIP, human is a peptide hormone consisting of 42 amino acids that also acts as a promoter of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. In addition, GIP, human acts as an enteric proinsulin hormone released by intestinal K cells in response to nutrient intake. |
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NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects. |
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