PQ 401

For research use only.

Catalog No.S8003

3 publications

PQ 401 Chemical Structure

CAS No. 196868-63-0

PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.

Selleck's PQ 401 has been cited by 3 publications

3 Customer Reviews

  • IGF-1R is key determinant of the EI24-mediated gefitinib sensitivity. (A and B) EI24-knockdown cells were treated with the indicated concentrations of inhibitorsfor 24 h before cell viability was measured by the MTT assay. Error bars, S.D., p-values were calculated using unpaired t-test.*p < 0.01,**p = 0.0003,***p < 0.0001. (C and D)EI24-knockdown cells were fixed and stained with crystal violet after 14 days treatment with concentrations of gefitinib (0.1 M), PQ401 (5 M), and AG1024 (20 M). (Eand F) Kaplan–Meier survival plots were obtained using Kaplan–Meier Plotter and display the probability of overall survival of lung cancer patients grouped according toEI24 (208289 s at, E) and IGF-1R (203627 at, F) expression. p-Values were calculated using the log-rank test.

    Lung Cancer, 2015, 90(2):175-81. PQ 401 purchased from Selleck.

    Jurkat cells were pretreated with 10 μM of PQ401 (IGF-1R inhibitor) for 60 min and then were co-treated with everolimus (40 nM) for the indicated times.

    Acta Pharmacol Sin, 2018, 39(12):1894-1901. PQ 401 purchased from Selleck.

  • PQ401 induces apoptosis in glioma cells. (A) U87MG cells were treated with PQ401 at the indicated concentrations for 48 hours, followed by PI staining and flow cytometry analysis. * indicates P < 0.05 by one-way ANOVA followed by Dunnet's test for comparisons between PQ401 treatments with various doses and no PQ401 treatment group. (B) U87MG cells were incubated with PQ401 for 48 hours. The nuclei were stained with Hoechst and analyzed using a fluorescent microscope. The representative images are presented. (C) The number of cells with condensed/fragmented nuclei was quantitated by counting in seven random fields and the inhibition was calculated. * indicates P < 0.05 by one-way ANOVA followed by Dunnet's test for comparisons between PQ401 treatments with various doses and no PQ401 treatment group.

    J Chemother, 2016, 28(1):44-9.. PQ 401 purchased from Selleck.

Purity & Quality Control

Choose Selective IGF-1R Inhibitors

Biological Activity

Description PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
Targets
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. PQ 401 significantly reduced proliferation of MCF-7 cells with IC50 of 8 μM. PQ 401 also inhibits growth of MCNeuA cells with IC50 of 15 μM. PQ 401 inhibits the IGF-I-mediated antiapoptotic pathway in MCF-7 cells. PQ 401 increases caspase-mediated apoptotic activity in MCF-7 cells. [1]
In vivo PQ 401 (50 mg/Kg, 100 mg/Kg) significantly inhibits MCNeuA tumor growth in a dose-dependent manner. [1]

Protocol

Kinase Assay:[1]
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IGF-IR Peptide Autophosphorylation:

One microgram of constitutively active IGF-IR kinase domain peptide isincubated +/− varying concentrations of PQ 401 in 2% DMSO in 40 mM Tris (pH 7.4), 80μMEGTA, 0.25% 2-mercaptoethanol, 80μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP isthen added at a final concentration of 20μM. Autophosphorylation of the kinase domain peptide isallowed to occur for 20 minutes at 22℃. The reaction isstopped by the addition of SDS-reducing buffer and the samples are run on SDS-PAGE. Following transfer to nitrocellulose membrane, peptide autophosphorylation isdetermined by Western blotting employing an antibody against phosphotyrosine (PY20).
Cell Research:[1]
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  • Cell lines: MCF-7, MCNeuA
  • Concentrations: ~50 μM
  • Incubation Time: 3 days
  • Method: The inhibitory effects of diaryl urea on breast cancer cell growth are determined using a CyQuant cell proliferation assay kit. MCF-7 or MCNeuA cells are plated in 96-well plates (5 × 103 per well) in phenol red-free DMEM supplemented with 10% FCS. One plate isprepared for each harvest day. Cells are allowed to adhere overnight and are then treated with various concentrations of diaryl urea or DMSO as a vehicle control. Microplate cultures are harvested on days 0, 1, 2, and 3 by inverting the microplate onto paper towels with gentle blotting to remove growth medium without disrupting adherent cells. Each plate iskept at −80 ℃ until the end of the experiment (day 3) when all of the plates are thawed and assayed together. After thawing, 200 μL of CyQuant GR solution are added to each well and the plates are incubated in the dark for 2 to 5 minutes. Fluorescence ismeasured with a SpectraMax Gemini XS fluorescence microplate reader with 480-nm excitation and 520-nm emission. Proliferation index iscalculated as the percent of nucleotide content versus control cells at day 0.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: FVB/N-TgN(MMTVneu)202 mouse injected with MCNeuA cells.
  • Dosages: 50 or 100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 32 mg/mL (93.62 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing. 		5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 341.79
Formula

C18H16ClN3O2
CAS No. 196868-63-0
Storage powder
in solvent
Synonyms N/A
Smiles CC1=NC2=CC=CC=C2C(=C1)NC(=O)NC3=C(C=CC(=C3)Cl)OC

In vivo Formulation Calculator (Clear solution)

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

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID