Zibotentan (ZD4054)

ChemicalBook > CAS DataBase List > Zibotentan (ZD4054)

Product Name: Zibotentan (ZD4054)
CAS No.: 186497-07-4
Chemical Name: Zibotentan (ZD4054)
Synonyms: ZD454;Zd4054;CS-558;Zd 4054;Zibotentan;Zibotentan(ZD4054);zibotentan,CID 9910224;ZD4054;ZD-4054;ZD 4054;Zibotentan >=98% (HPLC);ZIBOTENTAN (ZD4054) 250MG
CBNumber: CB31475871
Molecular Formula: C19H16N6O4S
Formula Weight: 424.43
MOL File: 186497-07-4.mol

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Zibotentan (ZD4054) Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning
Hazard statements: H302Harmful if swallowed

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 23702
Product name: Zibotentan
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 23702
Product name: Zibotentan
Purity: ≥98%
Packaging: 5mg
Price: $93
Updated: 2024/03/01

Cayman Chemical

Product number: 23702
Product name: Zibotentan
Purity: ≥98%
Packaging: 10mg
Price: $169
Updated: 2024/03/01

Cayman Chemical

Product number: 23702
Product name: Zibotentan
Purity: ≥98%
Packaging: 25mg
Price: $381
Updated: 2024/03/01

TRC

Product number: Z359900
Product name: Zibotentan
Packaging: 10mg
Price: $120
Updated: 2021/12/16

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Zibotentan (ZD4054) Chemical Properties,Usage,Production

Description

Zibotentan is a selective antagonist of the endothelin (ET) receptor type A (IC₅₀s = 21 and >10,000 nM for human recombinant ET_A and ET_B, 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

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

Raw materials

Preparation Products

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186497-07-4, Zibotentan (ZD4054)Related Search:

macitentan Aprepitant VX-770 Sitaxentan sodium Entinostat Rapamycin Zibotentan (ZD4054) 2-Amino-3-methoxy-5-methylpyrazine

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

ZD454

ZIBOTENTAN (ZD4054);ZD4054;ZD-4054;ZD 4054

ZIBOTENTAN (ZD4054) 250MG

zibotentan,CID 9910224

ZD4054;ZD-4054;ZD 4054

CS-558

3-Pyridinesulfonamide, N-(3-methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-

Zibotentan >=98% (HPLC)

Zibotentan (ZD4054) USP/EP/BP

Zibotentan ZD4054 ZD-4054

186497-07-4

C19H16N6O4S

Inhibitors