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Proteases/Proteasome Serine Protease Upamostat

Upamostat

Catalog No. T13257   CAS 590368-25-5
Synonyms: WX-671

Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.

Upamostat, CAS 590368-25-5
Pack Size Availability Price/USD Quantity
1 mg In stock 136.00
5 mg In stock 277.00
10 mg In stock 415.00
25 mg In stock 755.00
50 mg In stock 1121.00
100 mg In stock 1682.00
1 mL * 10 mM (in DMSO) In stock 427.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Upamostat is an inhibitor of a serine protease and is a urokinase plasminogen activator (uPA) inhibitor.
Targets&IC50 Serine protease,  
In vitro Upamostat is an inhibitor of urokinase plasminogen activator (uPA). Upamostat is the oral prodrug of the active metabolite WX-UK1, a novel inhibitor of uPA [1]. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, and 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].
In vivo
Synonyms WX-671
Purity 98.80%
Molecular Weight 629.81
Formula C32H47N5O6S
CAS No. 590368-25-5

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 250 mg/mL (396.95 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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. 2. Froriep D, et al. Activation of the anti-cancer agent upamostat by the mARC enzyme system. Xenobiotica. 2013 Sep;43(9):780-4. 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.

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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.