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Purity: ≥98%
PQ401 (PQ-401) is a novel, potent and selective inhibitor of IGF-1R (insulin-like growth factor-1 receptor) with potential antineoplastic activity. At an IC50 of less than 1 μM, it inhibits IGF-1R. PQ-401 suppresses glioma cell growth, proliferation, and migration while inducing apoptosis. PQ 401 dramatically and dose-dependently inhibited the growth of MCNeuA tumors at two different dosages (50 mg/kg and 100 mg/kg).
| Targets |
IGF-IR; apoptosis
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
For twenty minutes, a single microgram of constitutively active IGF-IR kinase domain peptide is incubated +/− with different 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. At a final concentration of 20μM, ATP is then added. The kinase domain peptide is permitted to autophosphorylate for 20 minutes at 22°C. Samples are run on SDS-PAGE after SDS-reducing buffer is added to stop the reaction. Peptide autophosphorylation is assessed by Western blotting using an antibody against phosphotyrosine (PY20) after transfer to nitrocellulose membrane.
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| Cell Assay |
Using a CyQuant cell proliferation assay kit, the inhibitory effects of diaryl urea on the growth of breast cancer cells are ascertained. In 96-well plates (5 × 103 per well), MCF-7 or MCNeuA cells are plated in phenol red-free DMEM that has been supplemented with 10% FCS. There is a single plate ready for every harvest day. Following an overnight period of adhesion, cells are treated with varying concentrations of diaryl urea or, as a vehicle control, DMSO. On days 0, 1, 2, and 3, microplate cultures are harvested by gently blotting the microplate onto paper towels while inverting it to remove the growth medium without disturbing the adherent cells. Every plate is maintained at -80 °C until the third day of the experiment, when they are all thawed and analyzed collectively. Following thawing, 200 μL of CyQuant GR solution is added to each well, and the plates are then incubated for two to five minutes in the dark. Utilizing a SpectraMax Gemini XS fluorescence microplate reader with 480 nm excitation and 520 nm emission, fluorescence is measured. The nucleotide content percentage in comparison to control cells on day 0 is used to calculate the proliferation index.
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| Animal Protocol |
Female mice were MCNeuA tumor cells
50 or 100 mg/kg Administered i.p. thrice a week; 24 days |
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| References | ||
| Additional Infomation |
1-(5-chloro-2-methoxyphenyl)-3-(2-methyl-4-quinolinyl)urea is a member of quinolines.
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| Molecular Formula |
C18H16CLN3O2
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| Molecular Weight |
341.79
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| Exact Mass |
341.093
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| Elemental Analysis |
C, 63.25; H, 4.72; Cl, 10.37; N, 12.29; O, 9.36
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| CAS # |
196868-63-0
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| Related CAS # |
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| PubChem CID |
9549305
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
426.1±45.0 °C at 760 mmHg
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| Melting Point |
190 °C(dec.)
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| Flash Point |
211.5±28.7 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.709
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| LogP |
5.35
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
437
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=CC(C)=NC2=CC=CC=C12)NC3=C(OC)C=CC(Cl)=C3
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| InChi Key |
YBLWOZUPHDKFOT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16ClN3O2/c1-11-9-15(13-5-3-4-6-14(13)20-11)21-18(23)22-16-10-12(19)7-8-17(16)24-2/h3-10H,1-2H3,(H2,20,21,22,23)
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| Chemical Name |
1-(5-chloro-2-methoxyphenyl)-3-(2-methylquinolin-4-yl)urea
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| Synonyms |
PQ-401; PQ 401; PQ401
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (4.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.43 mg/mL (4.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.43 mg/mL (4.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% propylene glycol: 5 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9258 mL | 14.6289 mL | 29.2577 mL | |
| 5 mM | 0.5852 mL | 2.9258 mL | 5.8515 mL | |
| 10 mM | 0.2926 mL | 1.4629 mL | 2.9258 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
PQ401 inhibits the IGF-I-mediated antiapoptotic pathway in MCF-7 cells. Mol Cancer Ther. 2006 Apr;5(4):1079-86. |
PQ401 increases caspase-mediated apoptotic activity in MCF-7 cells. Mol Cancer Ther. 2006 Apr;5(4):1079-86. |
Growth inhibition of MCNeuA cells in vivo by PQ401. Mol Cancer Ther. 2006 Apr;5(4):1079-86. |
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