Zibotentan (ZD4054)
Zibotentan (ZD4054; CAS 186497-07-4) is a selective antagonist of the endothelin A receptor (ET_AR). The endothelin-1 (ET-1)/ET_AR signaling axis is implicated in ovarian cancer progression. In vitro studies in ET_AR-positive human ovarian cancer cell lines demonstrate that Zibotentan decreases basal and ET-1-stimulated proliferation, suppresses phosphorylation of AKT and p42/44 MAPK, reduces anti-apoptotic protein bcl-2 expression, and elevates active caspase-3 levels, enhancing apoptosis. In vivo, Zibotentan inhibits tumor growth in HEY ovarian carcinoma xenograft models, reducing proliferation index, microvascular density, and MMP-2 expression, and augments paclitaxel's antitumor activity. Clinically, pharmacokinetic assessments in advanced solid tumor patients indicate consistent safety profiles across patient populations.
- 1. Qu L, Zhang X, et al. "Phenotypic assessment and ligand screening of ETA/ETB receptors with label-free dynamic mass redistribution assay." Naunyn Schmiedebergs Arch Pharmacol. 2019 Nov 28. PMID:31781785
- 2. Moody TW, Ramos-Alvarez I, et al. "Endothelin causes transactivation of the EGFR and HER2 in non-small cell lung cancer cells."j.peptides.2017.01.012. Epub 2017 Jan 31. PMID: 28153500
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 424.43 |
Cas No. | 186497-07-4 |
Formula | C19H16N6O4S |
Solubility | insoluble in EtOH; insoluble in H2O; ≥7.2 mg/mL in DMSO |
Chemical Name | N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide |
SDF | Download SDF |
Canonical SMILES | CC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | Zibotentan (ZD4054) is a specific antagonist of Endothelin (ET)A with an IC50 value of 21 nM. | |||||
Targets | ETA | |||||
IC50 | 21 nM |
Quality Control & MSDS
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Chemical structure

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