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PQ401

Cat. No. M2025
PQ401 Structure
Size Price Availability Quantity
10mg USD 105 In stock
50mg USD 320 In stock
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Quality Control
Biological Activity

PQ 401 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.

Protocol
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 (Sigma) 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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 341.79
Formula C18H16ClN3O2
CAS Number 196868-63-0
Purity 99.89%
Solubility DMSO
Storage at -20°C
References

Activation of the insulin-like growth factor-1 receptor induces resistance to epidermal growth factor receptor antagonism in head and neck squamous carcinoma cells.
Jameson MJ, et al. Mol Cancer Ther. 2011 Nov;10(11):2124-34. PMID: 21878657.

Autocrine loop for IGF-I receptor signaling in SLUG-mediated epithelial-mesenchymal transition.
Sivakumar R, et al. Int J Oncol. 2009 Feb;34(2):329-38. PMID: 19148466.

Diarylureas are small-molecule inhibitors of insulin-like growth factor I receptor signaling and breast cancer cell growth.
Gable KL, et al. Mol Cancer Ther. 2006 Apr;5(4):1079-86. PMID: 16648580.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PQ401 supplier, IGF-1R, inhibitors

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