Reagents and instruments for immunology, cell biology and molecular biology.

Linsitinib [867160-71-2]

Print

Cat# NB-64-30614-5mg

Size : 5mg

Brand : Neo Biotech

Request more information

Remove All

Linsitinib

(Synonyms: OSI-906) Copy Product Info

Synonyms: OSI-906

Catalog No. T6017 Copy Product Info

Purity: 99.92%

Linsitinib (OSI-906) belongs to small molecule inhibitors and is a dual IGF-1/IR inhibitor (IC50 = 35 and 75 nM, respectively) with selectivity, cell permeability, and oral activity. This compound is used in antitumor research and can effectively inhibit cell proliferation and induce apoptosis.

Cas No. 867160-71-2

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

Select Batch

Purity:99.92%

Color:White to Yellow

Product Introduction

Bioactivity

Description	Linsitinib (OSI-906) belongs to small molecule inhibitors and is a dual IGF-1/IR inhibitor (IC50 = 35 and 75 nM, respectively) with selectivity, cell permeability, and oral activity. This compound is used in antitumor research and can effectively inhibit cell proliferation and induce apoptosis.
Targets & IC50	IGF-1R:35 nM, Insulin Receptor:75 nM, IRR:75 nM
In vitro	Methods: In SW48 colon cancer cells, pretreatment with Linsitinib (1.0 or 10.0 μmol/L) for 48 hours was followed by treatment with Regorafenib (5 μmol/L) for 96 hours. Results: MTT assay showed cell viability decreased to 42±7%, indicating that Linsitinib could inhibit Regorafenib resistance.[1] Methods: In PC9, HCC827, and H1975 human lung cancer cells, treatment with Linsitinib (10 μmol/L) for 5 days inhibited cell proliferation as detected by MTT assay. Results: Combination with Gefitinib synergistically inhibited cell viability in PC9 and HCC827 cells and increased apoptosis rates in HCC827 and H1975 cells. Western blot confirmed that the mechanism involved inhibition of IGF-1R and downstream AKT/ERK phosphorylation. [2] Methods: In H295R and HAC15 human adrenocortical carcinoma cells, treatment with Linsitinib for 3 or 6 days resulted in dose- and time-dependent inhibition of cell proliferation as measured by DNA content. Results: IC50 values were 1.5×10⁻⁷ M and 2.9×10⁻⁸ M, respectively. Additionally, DNA fragmentation assay confirmed its ability to induce apoptosis.[3]
In vivo	Methods: In an AOM/DSS-induced C57BL/6J mouse colon cancer model, Linsitinib was orally administered in combination with Regorafenib. Results: The combination therapy significantly inhibited body weight loss, reduced tumor number (minimum 1±1), and prolonged survival (40%). [1]
Synonyms	OSI-906
Kinase Assay	Protein kinase biochemical assays: Protein kinase assays are either performed in-house by ELISA-based assay methods (IGF-1R,IR,EGFR and KDR) or at Upstate Inc.by a radiometric method with ATP at 100 μM concentration.In-house ELISA assays use poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates and phosphorylation is detected using an antiphosphotyrosine antibody conjugated to horseradish peroxidase.The bound antibody is quantified using ABTS as the peroxidase substrate by measuring absorbance at 405 / 490 nm.All assays use purified recombinant kinase catalytic domains.Recombinant enzymes of human IGF-1R or EGFR are expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and are purified in house.IC50 values are determined from the sigmoidal dose–response plot of percent inhibition versus log10 compound concentration.A minimum of three measurements,performed in duplicate,are carried out with in-house assays unless otherwise indicated.OSI-906 at a concentration of 1 μM is profiled versus a panel of kinases using the ProfilerProTM Kinase Selectivity Assay Kit.
Cell Research	For assays of cell proliferation, cells are seeded into 96-well plates in appropriate media containing FCS 10% and incubated for 3 days in the presence of OSI-906 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of intracellular ATP content using CellTiterGlo. Data is presented as a fraction of maximal proliferation, calculated by dividing the cellular density in the presence of varying concentrations of OSI-906 by the cellular density of control cells treated with vehicle (DMSO) only.(Only for Reference)

Chemical Properties

Molecular Weight	421.49
Formula	C₂₆H₂₃N₅O
Cas No.	867160-71-2
Smiles	NC=1C=2N(C(=NC2C3=CC4=C(C=C3)C=CC(=N4)C5=CC=CC=C5)[C@H]6C[C@@](C)(O)C6)C=CN1
Relative Density.	1.39 g/cm3

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 96 mg/mL (227.76 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.83 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3725 mL	11.8627 mL	23.7254 mL	118.6268 mL
5 mM	0.4745 mL	2.3725 mL	4.7451 mL	23.7254 mL
10 mM	0.2373 mL	1.1863 mL	2.3725 mL	11.8627 mL
20 mM	0.1186 mL	0.5931 mL	1.1863 mL	5.9313 mL
50 mM	0.0475 mL	0.2373 mL	0.4745 mL	2.3725 mL
100 mM	0.0237 mL	0.1186 mL	0.2373 mL	1.1863 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

OSI906OSI 906LinsitinibIRRInsulin ReceptorInhibitorinhibitIGF-1RIGF1R

Related Tags: Linsitinib chemical structure | Linsitinib in vivo | Linsitinib in vitro | Linsitinib formula | Linsitinib molecular weight