| Name | PQ401 |
| Description | PQ401 (IGF-1R Inhibitor II) suppresses autophosphorylation of IGF-1R domain(IC50<1 μM). |
| Cell Research | 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) |
| Kinase Assay | 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), 80 μMEGTA, 0.25% 2-mercaptoethanol, 80 μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP isthen added at a final concentration of 20 μM. 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). |
| In vivo | Treated mice received 50 or 100 mg/kg PQ401 prepared in 8% polysorbate 80/ethanol/PBS, administered i.p. thrice a week. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 8.5 mg/mL (24.87 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (2.93 mM), Sonication is recommended.
DMSO : 17.1 mg/mL (50.03 mM), Sonication is recommended.
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| Keywords | PQ-401 | PQ401 | PQ 401 | MCF-7 | Inhibitor | inhibit | IGF-1R | IGF1R | cells | caspase | cancer | breast | autophosphorylation | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Diabetic Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
