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Zibotentan (ZD4054) (Synonyms: ZD 4054)

Catalog No.GC16862

Zibotentan (ZD4054) (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM.

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Zibotentan (ZD4054) Chemical Structure

Cas No.: 186497-07-4

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Sample solution is provided at 25 µL, 10mM.

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Background

ZD4054 is a specific antagonist of the endothelin A receptor.

The autocrine endothelin (ET)-1/endothelin A receptor (ETAR) pathway is an important regulator of several processes involved in ovarian cancer progression.

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].

Clinical trial: The PK and safety profiles of ZD4054 determined in this Chinese patient population are similar to those previously reported. Findings suggest no clinically relevant inter-ethnic differences in ZD4054 disposition between the patient populations analyzed [3].

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.

Chemical Properties

Cas No. 186497-07-4 SDF
Synonyms ZD 4054
Chemical Name N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
Canonical SMILES CC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4
Formula C19H16N6O4S M.Wt 424.43
Solubility ≥ 7.2mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3561 mL 11.7805 mL 23.561 mL
5 mM 0.4712 mL 2.3561 mL 4.7122 mL
10 mM 0.2356 mL 1.1781 mL 2.3561 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 5 reference(s) in Google Scholar.)

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