Linsitinib

Name: Linsitinib
Brand: Tocris Bioscience
SKU: 7652

Tocris Bioscience, part of Bio-Techne | Catalog # 7652

Citations (3)

COA / SDS

Potent and selective dual inhibitor of the IGF-1 receptor and insulin receptor

Key Product Details

Description:	Potent and selective dual inhibitor of the IGF-1 receptor and insulin receptor
Chemical Name:	cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol
Purity:	≥98% (HPLC)
Molecular Weight:	421.49

View Full Technical Details for Linsitinib

Technical Data
Citations

Biological Activity for Linsitinib

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.

Compound Libraries for Linsitinib

Linsitinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Linsitinib

M. Wt	421.49
Formula	C₂₆H₂₃N₅O
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	867160-71-2
PubChem ID	11640390
InChi Key	PKCDDUHJAFVJJB-VLZXCDOPNA-N
Smiles	NC=1C=2N(C(=NC2C3=CC4=C(C=C3)C=CC(=N4)C5=CC=CC=C5)[C@]6(C[C@@](C)(O)C6)[H])C=CN1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Linsitinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	42.15	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for Linsitinib

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