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  5. Tocris Bioscience™ Linsitinib

Tocris Bioscience™ Linsitinib
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Catalog No. 765250
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Quantity:
10 mg
50 mg
This item is not returnable. View return policy
This item is not returnable. View return policy

Description

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

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.

Specifications

Chemical Name or Material cis-3-[8-Amino-1-(2-phenyl-7-quinolinyl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutanol
CAS 867160-71-2
Quantity 50 mg
Target IGF-I R/IGF1R
Molecular Formula C26H23N5O
Purity 0.98
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