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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% (HPLC)
Literature (3)
Pathways (1)

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.

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
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 Data for Linsitinib

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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 et al (2009) Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med.Chem. 1 1153 PMID: 21425998

If you know of a relevant reference for Linsitinib, please let us know.

View Related Products by Product Action

View all Insulin and Insulin-like Receptor Inhibitors

Keywords: Linsitinib, Linsitinib supplier, potent, selective, inhibitors, inhibits, IGF-1, receptors, insulin-like, anti-tumor, growth, factor, Insulin, and, Receptors, 7652, Tocris Bioscience

Citations for Linsitinib

Citations are publications that use Tocris products.

Currently there are no citations for Linsitinib. Do you know of a great paper that uses Linsitinib from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Kinases Product Listing

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for Linsitinib

Insulin Signaling Pathway

Insulin Signaling Pathway

Signaling through the insulin pathway is fundamental for the regulation of intracellular glucose levels. This pathway can become dysregulated in diabetes.