NAZ2329
Based on 3 publication(s) in Google Scholar
NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.14%
- No. CAS: 2809469-05-2
- Fòrmula: C21H18F3NO4S3
- Peso molecular:501.56
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) NAZ2329
More
Actividad biológica
IC50: 7.5 µM (PTPRZ), 4.8 µM (PTPRG), 35.7 µM (PTPRA), 56.7 µM (PTPRM), 23.7 µM (PTPRS), 35.4 µM (PTPRB), 15.2 µM (PTPN6), 14.5 µM (PTPN1)[1]
NAZ2329 (0-25 μM; 48 hours) dose-dependently inhibits cell proliferation and migration in all cell lines (rat glioblastoma cells bearing C6 clone and human U251 glioblastoma cells) [1].
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NAZ2329 (25 μM; 0-90 min) obviously promotes the phosphorylation level of paxillin at Tyr-118 site, leading to inhibition for PTPR substrate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rat glioblastoma cells bearing C6 clone, human U251 glioblastoma cells
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Concentration:0 µM, 6.3 µM, 12.5 µM, 25 µM
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Incubation Time:48 hours
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Result:Exerted inhibition in cell proliferation and migration in a dose-dependent manner.
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Cell Line:Rat glioblastoma cells bearing C6 clone
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Concentration:25 µM
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Incubation Time:0 min, 15 min, 30 min, 60 min, 90min
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Result:Promoted the phosphorylation level of paxillin at Tyr-118 site.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c- nu/nu mice aged 4 week-old bearing parental or Ptprz-knockdown C6 cells[1]
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Dosage:22.5 mg/kg; Temozolomide (TMZ, 50 mg/kg)
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Administration:Intraperitoneal injection; twice per week; 40 days
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Result:The combination of NAZ2329 and TMZ significantly delayed tumor growth compared to NAZ2329 or TMZ alone.
Chemical Information
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No. CAS 2809469-05-2
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Appearance Solid
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Peso molecular 501.56
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Fòrmula C21H18F3NO4S3
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Color White to off-white
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SMILES
CCOC1=C(CSC2=C(C(NS(=O)(C3=CC=CC=C3)=O)=O)SC=C2)C=C(C(F)(F)F)C=C1
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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
Publications (3)
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Journal Impact Factor
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Most Recent
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Oncogene
PTPRZ1 dephosphorylates and stabilizes RNF26 to reduce the efficacy of TKIs and PD-1 blockade in ccRCC. [Abstract]2024 Dec;43(50):3633-3644. PMID: 39443724 -
Cancers (Basel)
Integrin α6β4 Upregulates PTPRZ1 Through UCHL1-Mediated Hif-1α Nuclear Accumulation to Promote Triple-Negative Breast Cancer Cell Invasive Properties. [Abstract]2024 Oct 31;16(21):3683. PMID: 39518121 -
Solvente y solubilidad
DMSO : 100 mg/mL (199.38 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 (4.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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 (4.98 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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 (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 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 | 1.9938 mL | 9.9689 mL | 19.9378 mL | 49.8445 mL |
| 5 mM | 0.3988 mL | 1.9938 mL | 3.9876 mL | 9.9689 mL | |
| 10 mM | 0.1994 mL | 0.9969 mL | 1.9938 mL | 4.9844 mL | |
| 15 mM | 0.1329 mL | 0.6646 mL | 1.3292 mL | 3.3230 mL | |
| 20 mM | 0.0997 mL | 0.4984 mL | 0.9969 mL | 2.4922 mL | |
| 25 mM | 0.0798 mL | 0.3988 mL | 0.7975 mL | 1.9938 mL | |
| 30 mM | 0.0665 mL | 0.3323 mL | 0.6646 mL | 1.6615 mL | |
| 40 mM | 0.0498 mL | 0.2492 mL | 0.4984 mL | 1.2461 mL | |
| 50 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.9969 mL | |
| 60 mM | 0.0332 mL | 0.1661 mL | 0.3323 mL | 0.8307 mL | |
| 80 mM | 0.0249 mL | 0.1246 mL | 0.2492 mL | 0.6231 mL | |
| 100 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.4984 mL |
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