Linsitinib

Catalog # Availability Size / Price Qty
7652/50
7652/10
Linsitinib | CAS No. 867160-71-2 | IGF-I R/IGF1R
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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%

Product Details
Citations (1)
Reviews

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

M.Wt:
421.49
Formula:
C26H23N5O
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
867160-71-2

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.

Product Datasheets

Citation for Linsitinib

The citations listed below are publications that use Tocris products. Selected citations for Linsitinib include:

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