PQ401
Based on 2 publication(s) in Google Scholar
PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.85%
- No. CAS: 196868-63-0
- Fòrmula: C18H16ClN3O2
- Peso molecular:341.79
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PQ401
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Customer Validation & Images
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Actividad biológica
Descripciòn
IC50 & Target
IGF-IR; apoptosis[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BJ | EC50 |
>25 μM
Compound: 4{13,1}
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Cytotoxicity against human BJ cells after 72 hrs by Cell titer-glo assay
Cytotoxicity against human BJ cells after 72 hrs by Cell titer-glo assay
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[PMID: 21243104] |
| HEK293 | EC50 |
>25 μM
Compound: 4{13,1}
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Cytotoxicity against human HEK293 cells after 72 hrs by Cell titer-glo assay
Cytotoxicity against human HEK293 cells after 72 hrs by Cell titer-glo assay
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[PMID: 21243104] |
| HepG2 | EC50 |
>25 μM
Compound: 4{13,1}
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Cytotoxicity against human HepG2 cells after 72 hrs by Cell titer-glo assay
Cytotoxicity against human HepG2 cells after 72 hrs by Cell titer-glo assay
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[PMID: 21243104] |
| MCF7 | IC50 |
12 μM
Compound: K00614a, Quinolinyl-urea1
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Inhibition of IGF1R autophosphorylation in human MCF7 cells
Inhibition of IGF1R autophosphorylation in human MCF7 cells
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[PMID: 18077363] |
| MCF7 | IC50 |
15 μM
Compound: K00614a, Quinolinyl-urea1
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Growth inhibition of human MCF7 cells
Growth inhibition of human MCF7 cells
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[PMID: 18077363] |
| MCF7 | IC50 |
8 μM
Compound: K00614a, Quinolinyl-urea1
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Inhibition of IGF1R-dependent tumor cell growth in human MCF7 cells
Inhibition of IGF1R-dependent tumor cell growth in human MCF7 cells
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[PMID: 18077363] |
| MCF7 | IC50 |
<1 μM
Compound: 43
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Inhibition of IGF1R autophosphorylation in human MCF7 cells by Western blot analysis
Inhibition of IGF1R autophosphorylation in human MCF7 cells by Western blot analysis
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[PMID: 19610618] |
| MCF7 | IC50 |
12 μM
Compound: 43
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Inhibition of IGF1R autophosphorylation in human MCF7 cells by ELISA
Inhibition of IGF1R autophosphorylation in human MCF7 cells by ELISA
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[PMID: 19610618] |
| Raji | EC50 |
>25 μM
Compound: 4{13,1}
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Cytotoxicity against human Raji cells after 72 hrs by Cell titer-glo assay
Cytotoxicity against human Raji cells after 72 hrs by Cell titer-glo assay
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[PMID: 21243104] |
In Vitro
PQ401 (1, 5, 10, 25, and 50 μM; 3 days) inhibits proliferation of cultured MCF-7 cells grown in serum or IGF-I in MCF-7 cells[1].
Twenty-four hours of treatment with 15 μM PQ401 induces caspase-mediated apoptosis[1].
PQ401 inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC50 <1 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Breast cancer cells, MCF-7 cells
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Concentration:1, 5, 10, 25, and 50 μM
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Incubation Time:3 days
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Result:Significantly reduced proliferation (IC50, 8 μM) at concentrations in the range of 1 μM.
Produced a dramatic reduction in cell number from pretreatment levels at concentrations >10 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female mice were MCNeuA tumor cells[1]
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Dosage:50 or 100 mg/kg
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Administration:Administered i.p. thrice a week; 24 days
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Result:Resulted in a significant dose-dependent reduction in tumor growth. Tumor growth in the animals treated with 100 mg/kg was 20% of that in the vehicle-treated controls. This dosing protocol was well tolerated by the animals.
Chemical Information
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No. CAS 196868-63-0
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Appearance Solid
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Peso molecular 341.79
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Fòrmula C18H16ClN3O2
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Color White to light yellow
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Cancer
Short-term starvation reduces IGF-1 levels to sensitize lung tumors to PD-1 immune checkpoint blockade. [Abstract]2020 Jan;1(1):75-85. PMID: 35121837
PQ401 purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2020 Jan;1(1):75-85. [Abstract]
LLC cells cultured under normal or STS-like conditions in the presence of 1 µg/mL rIGF-1, PQ401 (500 ng/mL), their combination or vehicle. GAPDH was used as a control. This experiment was performed once.
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EMBO Mol Med
Myeloid p38α signaling promotes intestinal IGF-1 production and inflammation-associated tumorigenesis. [Abstract]2018 Jul;10(7):e8403. PMID: 29907597
Solvente y solubilidad
In Vitro:
DMSO : 14.29 mg/mL (41.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.43 mg/mL (4.18 mM); Clear solution
This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.43 mg/mL (4.18 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.43 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Pureza y Documentación
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Ficha de datos (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9258 mL | 14.6289 mL | 29.2577 mL | 73.1443 mL |
| 5 mM | 0.5852 mL | 2.9258 mL | 5.8515 mL | 14.6289 mL | |
| 10 mM | 0.2926 mL | 1.4629 mL | 2.9258 mL | 7.3144 mL | |
| 15 mM | 0.1951 mL | 0.9753 mL | 1.9505 mL | 4.8763 mL | |
| 20 mM | 0.1463 mL | 0.7314 mL | 1.4629 mL | 3.6572 mL | |
| 25 mM | 0.1170 mL | 0.5852 mL | 1.1703 mL | 2.9258 mL | |
| 30 mM | 0.0975 mL | 0.4876 mL | 0.9753 mL | 2.4381 mL | |
| 40 mM | 0.0731 mL | 0.3657 mL | 0.7314 mL | 1.8286 mL |
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