A selective ETA receptor antagonist
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Zibotentan

Item No. 23702

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3-methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide
CAS Number
186497-07-4
Synonyms
  • ZD 4054
Molecular Formula
C19H16N6O4S
Formula Weight
424.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:40): 0.02 mg/ml
λmax
265 nm
SMILES
CC1=NC(OC)=C(NS(C2=CC=CN=C2C3=CC=C(C4=NN=CO4)C=C3)(=O)=O)N=C1
InChi Code
InChI=1S/C19H16N6O4S/c1-12-10-21-17(19(23-12)28-2)25-30(26,27)15-4-3-9-20-16(15)13-5-7-14(8-6-13)18-24-22-11-29-18/h3-11H,1-2H3,(H,21,25)
InChi Key
FJHHZXWJVIEFGJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

    $420

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    Cayman Chemical
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    Product 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).1 It inhibits growth of HEY, OVCA 433, SKOV3, and A2780 cells induced by endothelin 1 (ET-1; Item No. 24127) in vitro.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Morris, C.D., Rose, A., Curwen, J., et al. Specific inhibition of the endothelin A receptor with ZD4054: Clinical and pre-clinical evidence. Br. J. Cancer 92(12), 2148-2152 (2005).

    2. Rosanò, L., Di Castro, V., Spinella, F., et al. 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. 6(7), 2003-2011 (2007).