| Identification | Back Directory | [Name]
Zibotentan (ZD4054) | [CAS]
186497-07-4 | [Synonyms]
ZD454
Zd4054
CS-558
Zd 4054
Zibotentan
Zibotentan(ZD4054)
zibotentan,CID 9910224
ZD4054;ZD-4054;ZD 4054
Zibotentan >=98% (HPLC)
ZIBOTENTAN (ZD4054) 250MG
Zibotentan (ZD4054) USP/EP/BP
ZIBOTENTAN (ZD4054);ZD4054;ZD-4054;ZD 4054
3-Pyridinesulfonamide, N-(3-methoxy-5-methylpyrazinyl)-2-(4-(1,3,4-oxadiazol-2-yl)phenyl)-
N-(3-METHOXY-5-METHYLPYRAZIN-2-YL)-2-[4-(1,3,4-OXADIAZOL-2-YL)PHENYL]PYRIDINE-3-SULFONAMIDE
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
3-Pyridinesulfonamide, N-(3-methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]- | [Molecular Formula]
C19H16N6O4S | [MDL Number]
MFCD09955343 | [MOL File]
186497-07-4.mol | [Molecular Weight]
424.43 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [Definition]
ChEBI: N-(3-methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide is a phenylpyridine. | [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]. | [target]
ETA | [storage]
Store at -20°C | [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. |
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| Company Name: |
China Langchem Inc.
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| Tel: |
0086-21-58956006 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList19141/0.htm |
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