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Zibotentan (ZD4054) is a more selective and specific endothelin-A receptor (ETAR) antagonist with an IC50 value of 21 nM. Zibotentan inhibits endothelin-1 (ET-1) mediated processes associated with cancer progression, including invasion, metastasis, and angiogenesis. Zibotentan has no demonstrable effect on the endothelin-B receptor (ETBR), which promotes apoptosis (cell death). It is intended to be used in combination with docetaxel as an addition to standard chemotherapy for patients with metastatic CRPC. Zibotentan (ZD4054) has been shown to compete with 125I-ET-1 for binding to the cloned human ETA-receptor in vitro. Zibotentan treatment produced significant inhibition of tumor growth in ovarian and breast xenografts.
| Cell Experiment | |
|---|---|
| Cell lines | OVCA 433 and HEY cells |
| Preparation method | Cell proliferation assay. [3H]thymidine incorporation was measured as previously described ( 5). Cells were seeded in 96-well plates at ∼80% confluence (2 × 106 per well) and incubated in serum-free medium for 24 h to induce quiescence and 100 nmol/L ET-1 was added. Responses to all treatments were assayed in sextuplicate, and results were expressed as the means of three separate experiments. |
| Concentrations | 1 μmol/L |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | HEY cells Xenografts in nude mice |
| Formulation | diluted in PBS |
| Dosages | 10 mg/kg/d for 21 days |
| Administration | i.p. |
| Molecular Weight | 424.43 |
| Formula | C19H16N6O4S |
| CAS Number | 186497-07-4 |
| Solubility (25°C) | DMSO 18 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Endothelin Receptor Products |
|---|
| Ambrisentan
Ambrisentan is an orally active, highly selective antagonist of the endothelin-1 type A receptor. |
| Sitaxsentan sodium
Sitaxsentan (TBC-11251) is an orally active, highly selective antagonist of endothelin A receptors. |
| Macitentan
Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist. |
| Bosentan Hydrate
Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
| Bosentan
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
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