Toggle Nav
Close
  • Menu
  • Setting

Linsitinib

Catalog No.
A8334
IGF1R/IR inhibitor,potent and novel
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$88.00
In stock
Evaluation Sample
$30.00
In stock
5mg
$73.00
In stock
10mg
$101.00
In stock
50mg
$226.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Linsitinib (CAS 867160-71-2), also known as OSI-906, is a small-molecule inhibitor targeting both insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R) kinases. It exhibits potent inhibitory effects, with IC50 values of 75 nM against IR and 35 nM against IGF-1R. In vitro studies using the 3T3/hulGF-1R (LISN) cell line demonstrate that Linsitinib inhibits IGF-1R ligand-dependent autophosphorylation and downstream signaling via pERK1/2, pAKT, and p-p70S6K. It shows antiproliferative activity across multiple cancer cell lines and exhibits dose-dependent tumor growth inhibition in LISN xenograft animal models, supporting its utility in oncology research.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt421.51
Cas No.867160-71-2
FormulaC26H23N5O
SynonymsOSI 906; OSI-906; OSI906
Solubility≥21.08 mg/mL in DMSO; insoluble in H2O; ≥2.88 mg/mL in EtOH with gentle warming and ultrasonic
Chemical Name3-[8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl]-1-methylcyclobutan-1-ol
SDFDownload SDF
Canonical SMILESCC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment: [1]

Cell lines

HepG2, Hep3B, Huh-7, PLC/PRF/5, SNU-387 and SNU-423 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

3 μM, 20 hours

Applications

All 6HCCcell lines showed higher IR phosphorylation than IGF-1R, suggesting the significance of IR activity in HCC. Furthermore, all 3 HCC cell lines (HepG2, Hep3B, and HuH-7) that are sensitive to OSI-906 had much higher phosphorylation levels of both IGF-1R and IR than insensitive cell lines. This suggests that sensitivity to OSI-906 associates with activation of both IGF-1R and IR in HCC cell lines.

Animal experiment: [2]

Animal models

Female athymic nude mice injected with NCI-H292 or NCI-H441 cells

Dosage form

Oral administration, 60 mg/kg

Applications

The NCI-H292 xenografts (sensitive to OSI-906 treatment) show a significant decrease (p

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Zhao H, Desai V, Wang J, et al. Epithelial–Mesenchymal Transition Predicts Sensitivity to the Dual IGF-1R/IR Inhibitor OSI-906 in Hepatocellular Carcinoma Cell Lines. Molecular cancer therapeutics, 2012, 11(2): 503-513.

[2] McKinley E T, Bugaj J E, Zhao P, et al. 18FDG-PET predicts pharmacodynamic response to OSI-906, a dual IGF-1R/IR inhibitor, in preclinical mouse models of lung cancer. Clinical Cancer Research, 2011, 17(10): 3332-3340.

Biological Activity

Description OSI-906 (Linsitinib) is a selective inhibitor of IGF-1R with IC50 of 35 nM; modestly potent to InsR with IC50 of 75 nM.
Targets IGF-1R InsR        
IC50 35 nM 75 nM        

Quality Control

Chemical structure

Linsitinib

Related Biological Data

Linsitinib

Related Biological Data

Linsitinib

Related Biological Data

Linsitinib

Related Biological Data

Linsitinib