Home Protein Tyrosine Kinase IGF-1R inhibitor PQ 401

research use only

PQ 401 IGF-1R inhibitor

Cat.No.S8003

PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
PQ 401 IGF-1R inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 341.79

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S800301 DMSO]32 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.99%
99.99

Chemical Information, Storage & Stability

Molecular Weight 341.79 Formula

C18H16ClN3O2

 Storage (From the date of receipt)
CAS No. 196868-63-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=NC2=CC=CC=C2C(=C1)NC(=O)NC3=C(C=CC(=C3)Cl)OC

Solubility

In vitro
Batch:

DMSO : 32 mg/mL ( (93.62 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
IGF-1R [1]
<1 μM
In vitro
PQ 401 is an IGF-1R inhibitor and inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC50 <1μM. This compound significantly reduced proliferation of MCF-7 cells with IC50 of 8 μM. It also inhibits growth of MCNeuA cells with IC50 of 15 μM. This inhibitor blocks the IGF-I-mediated antiapoptotic pathway in MCF-7 cells. It increases caspase-mediated apoptotic activity in MCF-7 cells. [1]
Kinase Assay
IGF-IR Peptide Autophosphorylation
One microgram of constitutively active IGF-IR kinase domain peptide is incubated +/− varying concentrations of PQ 401 in 2% DMSO in 40 mM Tris (pH 7.4), 80 μM EGTA, 0.25% 2-mercaptoethanol, 80 μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP is then added at a final concentration of 20 μM. Autophosphorylation of the kinase domain peptide is allowed to occur for 20 minutes at 22℃. The reaction is stopped by the addition of SDS-reducing buffer and the samples are run on SDS-PAGE. Following transfer to nitrocellulose membrane, peptide autophosphorylation is determined by Western blotting employing an antibody against phosphotyrosine (PY20).
In vivo
PQ 401 (50 mg/Kg, 100 mg/Kg) significantly inhibits MCNeuA tumor growth in a dose-dependent manner. [1]
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map