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| Zibotentan (ZD4054) Basic information |
| Product Name: | Zibotentan (ZD4054) | | Synonyms: | N-(3-METHOXY-5-METHYLPYRAZIN-2-YL)-2-[4-(1,3,4-OXADIAZOL-2-YL)PHENYL]PYRIDINE-3-SULFONAMIDE;3-Pyridinesulfonamide, N-(3-methoxy-5-methylpyrazinyl)-2-(4-(1,3,4-oxadiazol-2-yl)phenyl)-;Zd 4054;Zd4054;Zibotentan;Zibotentan(ZD4054);N-(3-Methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide;2-(4-(1,3,4-oxadiazol-2-yl)phenyl)-N-(3-Methoxy-5-Methylpyrazin-2-yl)pyridine-3-sulfonaMide | | CAS: | 186497-07-4 | | MF: | C19H16N6O4S | | MW: | 424.43 | | EINECS: | | Product Categories: | Inhibitors | | Mol File: | 186497-07-4.mol |
| Zibotentan (ZD4054) Chemical Properties |
| Melting point | 239 - 241°C | | Boiling point | 637.0±65.0 °C(Predicted) | | density | 1.422 | | storage temp. | Sealed in dry,Store in freezer, under -20°C | | solubility | DMSO (Sparingly), Methanol (Slightly) | | form | Solid | | pka | 5.62±0.40(Predicted) | | color | White to Off-White |
| Zibotentan (ZD4054) Usage And Synthesis |
| Description | 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). It inhibits growth of HEY, OVCA 433, SKOV3, and A2780 cells induced by endothelin 1 (ET-1; ) in vitro. 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. | | Uses | Zibotentan is a specific endothelin-A receptor antagonist that is a potential candidate in the treatment of prostate cancer, bone metastasis and various other types of cancer. | | in vitro | in the human ovarian cancer etar positive cell lines, zd4054 effectively inhibited the basal and et-1-induced cell proliferation, with the inhibition of akt and p42/44mapk phosphorylation, and increased apoptosis, through the inhibition of bcl-2 and activation of caspase-3 and poly(adp-ribose) polymerase proteins. [1]. | | in vivo | in hey ovarian cancer xenografts, zd4054 inhibited tumor growth to the same degree as paclitaxel. moreover, zd4054-dependent tumor growth inhibition was associated with a reduction in proliferation index, mmp-2 expression, and microvessel microvessel density [2]. | | references | [1] morris cd, rose a, curwen j, hughes am, wilson dj, webb dj. 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] rosanò l, di castro v, spinella f, nicotra mr, natali pg, bagnato a. 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.[3] li j, liu y, qian j, wu l, kemp j, nii m, tomkinson h, zuo y, ranson m, usami m. single- and multiple-dose pharmacokinetics, safety and tolerability of zibotentan (zd4054) in chinese men with advanced solid tumors. cancer chemother pharmacol. 2012 jul;70(1):57-63. |
| Zibotentan (ZD4054) Preparation Products And Raw materials |
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