Linsitinib

Product Description

Linsitinib is a potent and selective dual inhibitor of the IGF-1 receptor (IC₅₀ = 35 nM) and insulin receptor (IC₅₀ = 75 nM); it inhibits ligand-dependent auto-phosphorylation of both receptor tyrosine kinases and prevents ligand-induced activation of downstream pathways including pAKT, pERK1/2 and p-p70S6K. The compound is selective for IGF-1R, IR and IRR in a panel of 88 kinases. Lisintinib inhibits proliferation in a variety of tumor cell lines and shows robust in vivo antitumor efficacy in an IGF-1R-driven LSN xenograft model. Orally bioavailable.

Solubility

Preparing Stock Solutions for Linsitinib

The following data is based on the product molecular weight 421.49

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.37 mL	11.86 mL	23.73 mL
5 mM	0.47 mL	2.37 mL	4.75 mL
10 mM	0.24 mL	1.19 mL	2.37 mL
50 mM	0.05 mL	0.24 mL	0.47 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Mulvihill Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med.Chem. 2009 PMID: 21425998