Linsitinib

Inhibitor of IGF1R, INSR, INSRR

Structure

Information

Protein target names: IGF1R, INSR, INSRR

Mechanism of action: Inhibitor

Recommended in-cell concentration:
100 - 1000 nM

In Vitro Validations

Uniprot ID: P08069
Target Class: Kinase
Target SubClass: TK
Potency: IC50
Potency Value: 35 nM
Potency Assay: In-house ELISA assays
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: Yes, see Future Chem paper
Target aliases:
Insulin-like growth factor 1 receptor, IGF1R, IGF1 ...

DOI Reference: 10.4155/fmc.09.89

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This is the best available probe for INSRR and IRR. A panel of 88 kinases was profiled when selectivity was assessed.

(last updated: 28 Jul 2017 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Linsitinib (OSI-906) has excellent kinase selectivity, and is quite potent against the indicated kinases that it does inhibit. It shows very good in vivo activity, and is orally bioavailable. Together, these properties make linsitinib a high-quality probe for INSR and IGF-1R activity in cells and in vivo.

(last updated: 10 Nov 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

This is a dual selective  IGF1R & INSR (and related INSRR) kinase inhibitor with demonstrated kinase selectivity an cell-based assay activity with oral bioavailability.

(last updated: 16 Nov 2020 )