JPM-OEt
Based on 3 publication(s) in Google Scholar
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.99%
- No. CAS: 262381-84-0
- Fòrmula: C20H28N2O6
- Peso molecular:392.45
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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) JPM-OEt
MoreVer todos los productos específicos de isoformas Cathepsin
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Actividad biológica
JPM-OEt (50 mg/kg; i.p.; twice daily for 4 weeks) leads to tumor regression in the RIP1-Tag2 (RT2) mouse model of pancreatic islet cell tumorigenesis[2].
JPM-OEt (50 mg/kg; i.p.; daily from 63 to 98 days) causes a significant delay in the increase of tumour burden during the first 2 weeks of treatment[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female mice of a transgenic mouse[3]
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Dosage:50 mg/kg
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Administration:i.p.; daily from 63 to 98 days
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Result:Caused a significant delay in the increase of tumour burden during the first 2 weeks of treatment. However, on days 84, 91 and 98 no significant differences between both groups could be detected.
Chemical Information
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No. CAS 262381-84-0
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Appearance Solid
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Peso molecular 392.45
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Fòrmula C20H28N2O6
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Color White to off-white
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SMILES
O=C([C@H]1O[C@@H]1C(N[C@H](C(NCCC2=CC=C(O)C=C2)=O)CC(C)C)=O)OCC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Clin Cancer Res
A Cathepsin-Targeted Quenched Activity-Based Probe Facilitates Enhanced Detection of Human Tumors during Resection. [Abstract]2022 Sep 1;28(17):3729-3741. PMID: 35792882 -
Sci Rep
Hepatitis C virus NS3/4A inhibitors and other drug-like compounds as covalent binders of SARS-CoV-2 main protease. [Abstract]2022 Jul 16;12(1):12197. PMID: 35842458 -
Mol Imaging
Preclinical Evaluation of an Activity-Based Probe for Intraoperative Imaging of Esophageal Cancer. [Abstract]2022 Jul 14:2022:5447290. PMID: 35903245
Solvente y solubilidad
DMSO : 125 mg/mL (318.51 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 (protect from light). 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 (protect from light). 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: ≥ 6.25 mg/mL (15.93 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (15.93 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Withana NP, et al. Cathepsin B inhibition limits bone metastasis in breast cancer. Cancer Res. 2012 Mar 1;72(5):1199-209. [Content Brief]
[2]. Bell-McGuinn KM, et al. Inhibition of cysteine cathepsin protease activity enhances chemotherapy regimens by decreasing tumor growth and invasiveness in a mouse model of multistage cancer. Cancer Res. 2007 Aug 1;67(15):7378-85. [Content Brief]
[3]. Schurigt U, et al. Trial of the cysteine cathepsin inhibitor JPM-OEt on early and advanced mammary cancer stages in the MMTV-PyMT-transgenic mouse model. Biol Chem. 2008 Aug;389(8):1067-74. [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 (protect from light). 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 | 2.5481 mL | 12.7405 mL | 25.4810 mL | 63.7024 mL |
| 5 mM | 0.5096 mL | 2.5481 mL | 5.0962 mL | 12.7405 mL | |
| 10 mM | 0.2548 mL | 1.2740 mL | 2.5481 mL | 6.3702 mL | |
| 15 mM | 0.1699 mL | 0.8494 mL | 1.6987 mL | 4.2468 mL | |
| 20 mM | 0.1274 mL | 0.6370 mL | 1.2740 mL | 3.1851 mL | |
| 25 mM | 0.1019 mL | 0.5096 mL | 1.0192 mL | 2.5481 mL | |
| 30 mM | 0.0849 mL | 0.4247 mL | 0.8494 mL | 2.1234 mL | |
| 40 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL | 1.5926 mL | |
| 50 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2740 mL | |
| 60 mM | 0.0425 mL | 0.2123 mL | 0.4247 mL | 1.0617 mL | |
| 80 mM | 0.0319 mL | 0.1593 mL | 0.3185 mL | 0.7963 mL | |
| 100 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6370 mL |
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