Home Protein Tyrosine Kinase IGF-1R inhibitor PQ 401

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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

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 32 mg/mL (93.62 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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

Mechanism of Action

Targets/IC50/Ki
IGF-1R
<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.
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.
References

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