Linsitinib
Chemical Name: cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol
Purity: ≥98%
Biological Activity
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.Technical Data
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.
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Citation for Linsitinib
The citations listed below are publications that use Tocris products. Selected citations for Linsitinib include:
1 Citation: Showing 1 - 1
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Epicardioid single-cell genomics uncovers principles of human epicardium biology in heart development and disease.
Authors: Meier Et al.
Nat Biotechnol 2023;
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