PDZ1i
Based on 1 Customer Validation
PDZ1i (113B7) is a inhibitor of MDA-9/Syntenin, with selective binding to the PDZ1 domain. PDZ1i inhibits radiation-induced invasion of glioblastoma (GBM) cells, radiosensitizes GBM cells, and impairs GBM-related signaling pathways (including Src/EphA2, EGFRvIII/FAK, and NF-κB). PDZ1i reduces radiation-induced secretion of invasion-related proteases (MMP-2, MMP-9, ADAM9). PDZ1i shows anti-tumor effects in nude mice bearing intracranial U1242-luc xenografts or GBM xenografts. PDZ1i can be used for the study of glioblastoma (GBM), breast cancer and prostate cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.29%
- No. CAS: 2083618-79-3
- Fòrmula: C28H26N8O4
- Peso molecular:538.56
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
PDZ1i (50 μM, 2 h) does not further radiosensitize immortalized primary human fetal astrocytes (Im-PHFAs) but markedly enhances radiosensitivity of U87 GBM cells, and significantly decreases proliferation of U87 cells when combined with radiation[1].
PDZ1i (50 μM, 2 h) abolishes radiation-induced invasion gains in U87 GBM cells[1].
PDZ1i (2 h) significantly reduces phospho-EGFR (Y845) levels in both non-radiated and radiated U87-EGFRvIII GBM cells, nullifies radiation-enhanced FAK activation (phospho-FAK Y576/577), and decreases radiation-induced NF-κB activation (phospho-p65) in U87-EGFRvIII cells[1].
PDZ1i disrupts the interaction between MDA-9/Syntenin and EGFR in both non-radiated and radiated GBM cells[1].
PDZ1i (50 μM, 2 h) reduces radiation-induced increases in the secretion of MMP-2, MMP-9, cathepsin family members, and ADAM9 in U1242 GBM cells[1].
PDZ1i (50 μM, 24 h) effectively crosses the human brain microvascular endothelial cell (HBMEC) barrier and inhibits the invasion of GBM6 cells, with comparable efficacy to direct pretreatment of GBM6 cells[1].
PDZ1i (5 μM) reduces the expression levels of CD44v3 and heparan sulfate (HS) on the surface of radiation-induced extracellular vesicles (IR-tEVs) derived from breast cancer MDA-MB-231 cells, and decreases the total production of IR-tEVs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87 GBM cells
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Concentration:50 μM
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Incubation Time:2 h
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Result:Abolished radiation-induced invasion gains in U87 GBM cells.
PDZ1i (30 mg/kg, i.p., 2 h before radiation, 4 consecutive days) shows enhanced anti-tumor effects when combined with radiation (2.5 Gy/day, 4 days) in nude mice bearing intracranial U1242-luc xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:GBM6 cells were intracranially implanted into nude mice[1]
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Dosage:30 mg/kg
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Administration:i.p., three times per week, 2 weeks
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Result:Demonstrated efficacy in reducing tumor size, increasing tumor demarcation, and extending survival.
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Animal Model:U1242-luc cells were intracranially implanted into nude mice under anesthesia[1]
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Dosage:30 mg/kg
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Administration:i.p., 2 h before radiation, 4 consecutive days
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Result:Showed enhanced anti-tumor effects when combined with radiation (2.5 Gy/day, 4 days).
Chemical Information
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No. CAS 2083618-79-3
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Appearance Solid
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Peso molecular 538.56
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Fòrmula C28H26N8O4
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Color White to off-white
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SMILES
O=C1N2C(NC3=C1CCC3)=NC(C(NC(C=C4C)=C(C=C4NC(CCC5=NN=C(C6=CC=CC=C6)O5)=O)C)=O)=N2
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Synonyms
113B7
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (185.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 2.5 mg/mL (4.64 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.64 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureza y Documentación
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Ficha de datos (277 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
[1]. Kegelman TP, et al. Inhibition of radiation-induced glioblastoma invasion by genetic and pharmacological targeting of MDA-9/Syntenin. Proc Natl Acad Sci U S A. 2017 Jan 10;114(2):370-375. [Content Brief]
[2]. Das D, et al. Suppression of Prostate Cancer Pathogenesis Using an MDA-9/Syntenin (SDCBP) PDZ1 Small-Molecule Inhibitor. Mol Cancer Ther. 2019 Nov;18(11):1997-2007. [Content Brief]
[3]. Clark GC, et al. Radiation induces ESCRT pathway dependent CD44v3+ extracellular vesicle production stimulating pro-tumor fibroblast activity in breast cancer. Front Oncol. 2022 Aug 29;12:913656. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8568 mL | 9.2840 mL | 18.5680 mL | 46.4201 mL |
| 5 mM | 0.3714 mL | 1.8568 mL | 3.7136 mL | 9.2840 mL | |
| 10 mM | 0.1857 mL | 0.9284 mL | 1.8568 mL | 4.6420 mL | |
| 15 mM | 0.1238 mL | 0.6189 mL | 1.2379 mL | 3.0947 mL | |
| 20 mM | 0.0928 mL | 0.4642 mL | 0.9284 mL | 2.3210 mL | |
| 25 mM | 0.0743 mL | 0.3714 mL | 0.7427 mL | 1.8568 mL | |
| 30 mM | 0.0619 mL | 0.3095 mL | 0.6189 mL | 1.5473 mL | |
| 40 mM | 0.0464 mL | 0.2321 mL | 0.4642 mL | 1.1605 mL | |
| 50 mM | 0.0371 mL | 0.1857 mL | 0.3714 mL | 0.9284 mL | |
| 60 mM | 0.0309 mL | 0.1547 mL | 0.3095 mL | 0.7737 mL | |
| 80 mM | 0.0232 mL | 0.1161 mL | 0.2321 mL | 0.5803 mL | |
| 100 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.4642 mL |
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