Upamostat

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[1].

Product Specifications

CAS Number

[590368-25-5]

Product Name Alternative

WX-671

UNSPSC

12352005

Hazard Statement

H228, H315, H319

Target

PAI-1; Ser/Thr Protease

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Infection

Assay Protocol

https://www.medchemexpress.com/Upamostat.html

Concentration

10mM

Purity

99.02

Solubility

DMSO : ≥ 250 mg/mL

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

Molecular Formula

C32H47N5O6S

Molecular Weight

629.81

Precautions

H228, H315, H319

References & Citations

[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.