PQ 401
Catalog No.S8003
Molecular Weight(MW): 341.79
PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
Cited by 3 Publications
3 Customer Reviews
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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.
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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. | ||
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| Targets |
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| 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] |
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| 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). |
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| Cell Research:[1] |
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| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 32 mg/mL (93.62 mM) |
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| 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 |
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| Formula | C18H16ClN3O2 |
| CAS No. | 196868-63-0 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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