A selective ETA receptor antagonist (IC50s = 21 and >10

Zibotentan – 1 mg

Brand:
Cayman
CAS:
186497-07-4
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Zibotentan is a selective antagonist of the endothelin (ET) receptor type A (IC50s = 21 and >10,000 nM for human recombinant ETA and ETB, respectively).{40680} It inhibits growth of HEY, OVCA 433, SKOV3, and A2780 cells induced by endothelin 1 (ET-1; Item No. 24127) in vitro.{40681} Zibotentan reduces ET-1-induced expression of MMP-2, MMP-9, VEGF, COX-1 and COX-2, mediators of cell invasion and angiogenesis, in HEY cells. In vivo, zibotentan (10-50 mg/kg per day) reduces tumor growth in an HEY mouse xenograft model in a dose-dependent manner. Formulations containing zibotentan are under clinical investigation for the treatment of ovarian and castration-resistant prostate cancers.  

 

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SKU: 23702 - 1 mg Category:

Description

A selective ETA receptor antagonist (IC50s = 21 and >10,000 nM for human recombinant ETA and ETB, respectively); inhibits ET-1-induced growth of HEY, OVCA 433, SKOV3, and A2780 cells in vitro; reduces ET-1-induced expression of MMP-2, MMP-9, VEGF, COX-1 and COX-2 in HEY cells; reduces tumor growth in an HEY mouse xenograft model in a dose-dependent manner (10-50 mg/kg per day)

Formal name: N-(3-methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide

Synonyms:  ZD 4054

Molecular weight: 424.4

CAS: 186497-07-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Migration & Metastasis

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