Zibotentan

Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research[1][2].

Product Specifications

CAS Number

[186497-07-4]

Product Name Alternative

ZD4054

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Endothelin Receptor

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer; Endocrinology

Assay Protocol

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

Purity

99.66

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=S(NC1=NC=C(C)N=C1OC)(C2=CC=CN=C2C3=CC=C(C4=NN=CO4)C=C3)=O

Molecular Formula

C19H16N6O4S

Molecular Weight

424.43

Precautions

H302, H315, H319, H335

References & Citations

[1]C D Morris, et al. Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br J Cancer. 2005 Jun 20;92 (12) :2148-52.|[2]Laura Rosanò, et al. Acquisition of chemoresistance and EMT phenotype is linked with activation of the endothelin A receptor pathway in ovarian carcinoma cells. Clin Cancer Res. 2011 Apr 15;17 (8) :2350-60.|[3]Laura Rosanò, et al. ZD4054, a specific antagonist of the endothelin A receptor, inhibits tumor growth and enhances paclitaxel activity in human ovarian carcinoma in vitro and in vivo. Mol Cancer Ther. 2007 Jul;6 (7) :2003-11.