Home Other Building Blocks 186497-07-4
186497-07-4,MFCD09955343
Catalog No.:AA00ABJB

186497-07-4 | Zibotentan (ZD4054)

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
≥98%
in stock  
$46.00   $32.00
- +
5mg
≥98%
in stock  
$133.00   $93.00
- +
10mg
97%
in stock  
$228.00   $160.00
- +
25mg
97%
in stock  
$385.00   $270.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00ABJB
Chemical Name:
Zibotentan (ZD4054)
CAS Number:
186497-07-4
Molecular Formula:
C19H16N6O4S
Molecular Weight:
424.4331
MDL Number:
MFCD09955343
SMILES:
COc1nc(C)cnc1NS(=O)(=O)c1cccnc1c1ccc(cc1)c1nnco1
Properties
Computed Properties
 
Complexity:
654  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
30  
Hydrogen Bond Acceptor Count:
10  
Hydrogen Bond Donor Count:
1  
Rotatable Bond Count:
6  
XLogP3:
1.4  

Downstream Synthesis Route
N-(isobutoxycarbonyl)-2-(4-methoxycarbonylphenyl)-N-(3-methoxy-5-methylpyrazin-2-yl)pyridine-3-sulphonamide 
  186497-07-4 

[1]Patent:US5866568,1999,A

[1]Patent:WO2007/10235,2007,A1.Locationinpatent:Page/Pagecolumn21

N-(isobutoxycarbonyl)N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-1,3,4-oxadiazol-2-ylphenyl)pyridine-3-sulphonamide 
  186497-07-4 

[1]Patent:WO2007/10235,2007,A1.Locationinpatent:Page/Pagecolumn6;20

[2]Patent:WO2007/10235,2007,A1.Locationinpatent:Page/Pagecolumn20-21

[1]Patent:WO2007/10235,2007,A1.Locationinpatent:Page/Pagecolumn22-23

Literature

Title: Identification of potent Yes1 kinase inhibitors using a library screening approach.

Journal: Bioorganic & medicinal chemistry letters 20130801

Title: Phase 3, randomized, placebo-controlled study of zibotentan (ZD4054) in patients with castration-resistant prostate cancer metastatic to bone.

Journal: Cancer 20121115

Title: The endothelin A receptor and epidermal growth factor receptor signaling converge on β-catenin to promote ovarian cancer metastasis.

Journal: Life sciences 20121015

Title: Optimizing the care of patients with advanced prostate cancer in the UK: current challenges and future opportunities.

Journal: BJU international 20120901

Title: Synthetic approaches and pharmacological activity of 1,3,4-oxadiazoles: a review of the literature from 2000-2012.

Journal: Molecules (Basel, Switzerland) 20120827

Title: Novel options for the treatment of castration-resistant prostate cancer.

Journal: World journal of urology 20120801

Title: Detection of previously unidentified metastatic disease as a leading cause of screening failure in a phase III trial of zibotentan versus placebo in patients with nonmetastatic, castration resistant prostate cancer.

Journal: The Journal of urology 20120701

Title: Single- and multiple-dose pharmacokinetics, safety and tolerability of zibotentan (ZD4054) in Chinese men with advanced solid tumors.

Journal: Cancer chemotherapy and pharmacology 20120701

Title: New developments in castrate-resistant prostate cancer.

Journal: BJU international 20120601

Title: Disposition and metabolism of the specific endothelin A receptor antagonist zibotentan (ZD4054) in healthy volunteers.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20120401

Title: Targeting the endothelin axis in prostate carcinoma.

Journal: Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine 20120401

Title: Castration-resistant prostate cancer: systemic therapy in 2012.

Journal: Clinics (Sao Paulo, Brazil) 20120401

Title: Interdisciplinary critique of sipuleucel-T as immunotherapy in castration-resistant prostate cancer.

Journal: Journal of the National Cancer Institute 20120222

Title: Emerging treatment options for patients with castration-resistant prostate cancer.

Journal: The Prostate 20120201

Title: Castration-resistant prostate cancer: mechanisms, targets, and treatment.

Journal: Prostate cancer 20120101

Title: Emerging targeted therapies for castration-resistant prostate cancer.

Journal: Frontiers in endocrinology 20120101

Title: Emerging therapies to prevent skeletal morbidity in men with prostate cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20110920

Title: Preliminary study of the specific endothelin a receptor antagonist zibotentan in combination with docetaxel in patients with metastatic castration-resistant prostate cancer.

Journal: The Prostate 20110901

Title: The disposition and metabolism of zibotentan (ZD4054): an oral-specific endothelin A receptor antagonist in mice, rats and dogs.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20110901

Title: Antiangiogenic agents and endothelin antagonists in advanced castration resistant prostate cancer.

Journal: European journal of cancer (Oxford, England : 1990) 20110801

Title: The metabolism of [14C]-zibotentan (ZD4054) in rat, dog and human, the loss of the radiolabel and the identification of an anomalous peak, derived from the animal feed.

Journal: Journal of pharmaceutical and biomedical analysis 20110601

Title: A phase II, randomized, multicenter study to assess the efficacy, safety, and tolerability of zibotentan (ZD4054) in combination with pemetrexed in patients with advanced non-small cell lung cancer.

Journal: Cancer chemotherapy and pharmacology 20110501

Title: Acquisition of chemoresistance and EMT phenotype is linked with activation of the endothelin A receptor pathway in ovarian carcinoma cells.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110415

Title: Emerging novel therapies in the treatment of castrate-resistant prostate cancer.

Journal: Canadian Urological Association journal = Journal de l'Association des urologues du Canada 20110401

Title: Castration-resistant prostate cancer: targeted therapies and individualized treatment.

Journal: The oncologist 20110301

Title: Current treatment strategies for castration-resistant prostate cancer.

Journal: Korean journal of urology 20110301

Title: A phase I study of zibotentan (ZD4054) in patients with metastatic, castrate-resistant prostate cancer.

Journal: Investigational new drugs 20110201

Title: Pharmacokinetics and tolerability of zibotentan (ZD4054) in subjects with hepatic or renal impairment: two open-label comparative studies.

Journal: BMC clinical pharmacology 20110101

Title: Progression of metastatic castrate-resistant prostate cancer: impact of therapeutic intervention in the post-docetaxel space.

Journal: Journal of hematology & oncology 20110101

Title: Therapeutic targets for bone metastases in breast cancer.

Journal: Breast cancer research : BCR 20110101

Title: Management Options in Advanced Prostate Cancer: What is the Role for Sipuleucel-T?

Journal: Clinical Medicine Insights. Oncology 20110101

Title: Docetaxel-based combination therapy for castration-resistant prostate cancer.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20101101

Title: Pharmacokinetic and tolerability profile of once-daily zibotentan (ZD4054) in Japanese and Caucasian patients with hormone-resistant prostate cancer.

Journal: International journal of clinical pharmacology and therapeutics 20101101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20101101

Title: Final safety and efficacy analysis of the specific endothelin A receptor antagonist zibotentan (ZD4054) in patients with metastatic castration-resistant prostate cancer and bone metastases who were pain-free or mildly symptomatic for pain: a double-blind, placebo-controlled, randomized Phase II trial.

Journal: BJU international 20101001

Title: ETAR antagonist ZD4054 exhibits additive effects with aromatase inhibitors and fulvestrant in breast cancer therapy, and improves in vivo efficacy of anastrozole.

Journal: Breast cancer research and treatment 20100901

Title: Zibotentan for the treatment of castrate-resistant prostate cancer.

Journal: Expert opinion on investigational drugs 20100701

Title: An open-label, randomized, single-center, two-period, phase I, crossover study of the effect of zibotentan (ZD4054) on the pharmacokinetics of midazolam in healthy male volunteers.

Journal: Clinical therapeutics 20100701

Title: Combination therapy of zibotentan with cisplatinum and paclitaxel is an effective regimen for epithelial ovarian cancer.

Journal: Canadian journal of physiology and pharmacology 20100601

Title: Update on castrate-resistant prostate cancer: 2010.

Journal: Current opinion in oncology 20100501

Title: [New drugs in metastatic castration-resistant prostate cancer].

Journal: Bulletin du cancer 20100101

Title: Critical appraisal of cabazitaxel in the management of advanced prostate cancer.

Journal: Clinical interventions in aging 20100101

Title: In vitro metabolism of the specific endothelin-A receptor antagonist ZD4054 and clinical drug interactions between ZD4054 and rifampicin or itraconazole in healthy male volunteers.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20090601

Title: Emerging therapies in castrate-resistant prostate cancer.

Journal: Current opinion in oncology 20090501

Title: ZD4054: a specific endothelin A receptor antagonist with promising activity in metastatic castration-resistant prostate cancer.

Journal: Expert opinion on investigational drugs 20080801

Title: Endothelin receptor antagonists in cancer therapy.

Journal: Cancer investigation 20071201

Title: Combined targeting of endothelin A receptor and epidermal growth factor receptor in ovarian cancer shows enhanced antitumor activity.

Journal: Cancer research 20070701

Title: Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence.

Journal: British journal of cancer 20050620

Quotation Request
Company Name:
*
Contact Person:
*
Email:
*
Quantity Required:
*
Country:
Additional Info:
SDS
Related Products of 186497-07-4
Tags:186497-07-4 Molecular Formula|186497-07-4 MDL|186497-07-4 SMILES|186497-07-4 Zibotentan (ZD4054)