Upamostat
Based on 2 publication(s) in Google Scholar
Upamostat (WX-671), a prodrug of WX-UK1, is an orally active serine protease inhibitor. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, blocking the plasminogen activation process mediated by it, thereby suppressing the invasion, migration and metastasis of tumor cells. Upamostat can be used in the research of metastatic breast cancer and locally advanced pancreatic cancer.
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- Pureté: 99.02%
- CAS No.: 590368-25-5
- Formule: C32H47N5O6S
- Masse moléculaire:629.81
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Upamostat
More
Activité biologique
Serine protease, uPA[1]
Upamostat is the urokinase plasminogen activator (uPA) inhibitor. Upamostat is the oral pro-drug of the active metabolite WX-UK1, a novel uPA inhibitor[1]. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, which plays a major role in tumor invasion and metastasis. Upamostat is the orally available amidoxime- (i.e. hydroxyamidine-) prodrug of the pharmacologically active form, WX-UK1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 590368-25-5
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Appearance Solid
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Masse moléculaire 629.81
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Formule C32H47N5O6S
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Color White to off-white
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SMILES
O=C(N1CCN(C([C@@H](NS(=O)(C2=C(C(C)C)C=C(C(C)C)C=C2C(C)C)=O)CC3=CC=CC(C(NO)=N)=C3)=O)CC1)OCC
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Synonyms
WX-671
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
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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Sci Adv
2021 Jun 18;7(25):eabf4885. PMID: 34144984 -
Solvant et solubilité
DMSO : ≥ 250 mg/mL (396.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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.
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.
Protocole
Rats[3]
Five 9-week old Sprague-Dawley rats are administered a single intravenous injection of 2 mg/kg of Upamostat. Upamostat is dissolved in a mixture of normal saline, dimethylacetamide, polyethylene glycol 400 and DMSO (3:3:3:1). Blood samples (0.15 mL) are taken serially for up to 10 h after drug administration and collected in heparinized centrifuge tubes. After centrifugation at 13,200 rpm for 10 min, the plasma samples are analyzed[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (544 KB)
- English - EN (544 KB)
- Français - FR (544 KB)
- Deutsch - DE (544 KB)
- Norwegian - NO (544 KB)
- Español - ES (544 KB)
- Swedish - SV (544 KB)
- Italian - IT (544 KB)
- Korean - KR (544 KB)
- Portuguese - PT (544 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Heinemann V, et al. Phase II randomised proof-of-concept study of the urokinase inhibitor upamostat (WX-671) in combination with gemcitabine compared with gemcitabine alone in patients with non-resectable, locally advanced pancreatic cancer. Br J Cancer. 2013 Mar 5;108(4):766-70. [Content Brief]
[2]. Froriep D, et al. Activation of the anti-cancer agent upamostat by the mARC enzyme system. Xenobiotica. 2013 Sep;43(9):780-4. [Content Brief]
[3]. Park C, et al. HPLC-MS/MS analysis of mesupron and its application to a pharmacokinetic study in rats. J Pharm Biomed Anal. 2018 Feb 20;150:39-42. [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, 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 |
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| DMSO | 1 mM | 1.5878 mL | 7.9389 mL | 15.8778 mL | 39.6945 mL |
| 5 mM | 0.3176 mL | 1.5878 mL | 3.1756 mL | 7.9389 mL | |
| 10 mM | 0.1588 mL | 0.7939 mL | 1.5878 mL | 3.9695 mL | |
| 15 mM | 0.1059 mL | 0.5293 mL | 1.0585 mL | 2.6463 mL | |
| 20 mM | 0.0794 mL | 0.3969 mL | 0.7939 mL | 1.9847 mL | |
| 25 mM | 0.0635 mL | 0.3176 mL | 0.6351 mL | 1.5878 mL | |
| 30 mM | 0.0529 mL | 0.2646 mL | 0.5293 mL | 1.3232 mL | |
| 40 mM | 0.0397 mL | 0.1985 mL | 0.3969 mL | 0.9924 mL | |
| 50 mM | 0.0318 mL | 0.1588 mL | 0.3176 mL | 0.7939 mL | |
| 60 mM | 0.0265 mL | 0.1323 mL | 0.2646 mL | 0.6616 mL | |
| 80 mM | 0.0198 mL | 0.0992 mL | 0.1985 mL | 0.4962 mL | |
| 100 mM | 0.0159 mL | 0.0794 mL | 0.1588 mL | 0.3969 mL |
Upamostat Related Classifications
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