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PQ401 is an IGF-1R inhibitor. PQ401 inhibits breast cancer cell growth in culture and in vivo. PQ401 inhibited autophosphorylation of the IGF-IR in cultured human MCF-7 cells with an IC50 of 12 micromol/L and autophosphorylation of the isolated kinase domain of the IGF-IR with an IC50 <1 micromol/L. In addition, PQ401 inhibited the growth of cultured breast cancer cells in serum at 10 micromol/L. PQ401 was even more effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 micromol/L). Treatment of MCF-7 cells with PQ401 was associated with a decrease in IGF-I-mediated signaling through the Akt antiapoptotic pathway. Twenty-four hours of treatment with 15 micromol/L PQ401 induced caspase-mediated apoptosis. In vivo, treatment with PQ401 (i.p. injection thrice a week) reduced the growth rate of MCNeuA cells implanted into mice. The IGF-1R tyrosine kinase inhibitor PQ401 inhibited growth of SCC-25 and Cal27 cells alone and also acted synergistically with gefitinib.
Oncotarget. 2017 Dec 28;9(12):10375-10387.
The crosstalk between breast carcinoma-associated fibroblasts and cancer cells promotes RhoA-dependent invasion via IGF-1 and PAI-1
PQ401 purchased from AbMole
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Source | Oncotarget (2017). Figure 6. PQ401 (Abmole Bioscience) |
| Method | intraperitoneally | |
| Cell Lines | SCID mice | |
| Concentrations | 50 mg/kg | |
| Incubation Time | 18 days | |
| Results | We found that the PQ401-treated group showed a 24% decrease in RhoA-GTP level in comparison to the control group |
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Source | Oncotarget (2017). Figure 5. PQ401 (Abmole Bioscience) |
| Method | intraperitoneally | |
| Cell Lines | SCID mice | |
| Concentrations | 50 mg/kg | |
| Incubation Time | 18 days | |
| Results | After 18 days of treatment, we did not observe any effect of PQ401, Y27632 or PQ401 combined with Y27632 on primary tumor growth, suggesting that the inhibition of ROCK or IGF-1 receptor did not affect cancer cell proliferation. |
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Source | J Chemother (2016). Figure 1. PQ401 |
| Method | cell viability assay | |
| Cell Lines | U87MG cells | |
| Concentrations | 5, 10 μM | |
| Incubation Time | 24, 48 or 72 h | |
| Results | Notably, PQ401 exhibited a dose- and treatment time-dependent inhibition on the growth of U87MG glioma cells, with an IC50 value of 5 μM |
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 cells |
| Preparation method | Effects of Diaryl Urea on IGF-I Stimulated Proliferation of Breast Cancer Cells MCF-7 cells were harvested by washing thrice with PBS and dissociating with 1 mL 0.05% trypsin. Cells were resuspended in 5 mL defined medium (1:1 Ham's F12/DMEM 4.5 g/L glucose; 1 mg/mL bovine serum albumin; 10 μg/mL transferrin; 15 mmol/L HEPES pH 7.2; 2 mmol/L L-glutamine; 100 units/mL penicillin G; 100 μg/mL streptomycin SO4; 2.5 μg/mL fungizone) containing 200 μg soybean trypsin inhibitor. Cells were plated in 96-well collagen-coated plates at a density of 5,000 per well in 100-μL medium. Twenty hours later, defined medium with or without IGF-I (10 nmol/L) was added. Four hours later, PQ401 diluted in defined medium was added. Plates were harvested on day 3, as described above, for determination of cell number by CyQuant assay. |
| Concentrations | 0, 2.5, 5, 7.5, 15, 30µM |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | MCNeuA tumor cells bearing mice model |
| Formulation | 8% polysorbate 80/ethanol/PBS |
| Dosages | 50 or 100 mg/kg |
| Administration | i.p. thrice a week |
| Molecular Weight | 341.79 |
| Formula | C18H16ClN3O2 |
| CAS Number | 196868-63-0 |
| Solubility (25°C) | DMSO 14 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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