1240299-33-5

Basic information

• Product Name: AZD3514
• Synonyms: AZD3514;1-[4-[2-[4-[1-[7,8-Dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-b]pyridazin-6-yl]-4-piperidinyl]phenoxy]ethyl]-1-piperazinyl]-ethanone;Ethanone, 1-[4-[2-[4-[1-[7,8-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-b]pyridazin-6-yl]-4-piperidinyl]phenoxy]ethyl]-1-piperazinyl]-;1-(4-(2-(4-(1-(3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)piperazin-1-yl)ethanone;1-(4-(2-(4-(1-(3-(Trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-
• CAS NO: 1240299-33-5
• Molecular Formula: C₂₅H₃₂F₃N₇O₂
• Molecular Weight: 519.5624896
• Product Categories: Inhibitors
• Mol File: 1240299-33-5.mol

Chemical Properties

• Boiling Point: 669.5±65.0 °C(Predicted)
• Appearance: /
• Density: 1.41±0.1 g/cm3(Predicted)
• Solubility: ≥24.45 mg/mL in DMSO; insoluble in H2O; ≥46.4 mg/mL in EtOH
• PKA: 6.31±0.10(Predicted)
• CAS DataBase Reference: AZD3514(CAS DataBase Reference)
• NIST Chemistry Reference: AZD3514(1240299-33-5)
• EPA Substance Registry System: AZD3514(1240299-33-5)

Safety Data

• Hazardous Substances Data: 1240299-33-5(Hazardous Substances Data)

Usage

Uses

Used in Oncology:
AZD3514 is used as a therapeutic agent for the treatment of hormone receptor-positive breast cancer and other hormone-dependent cancers. It targets the androgen receptor to inhibit the growth of cancer cells, offering a potential new treatment option for patients with these types of cancers.
Used in Clinical Trials:
AZD3514 is used as a subject of investigation in clinical trials to evaluate its safety, efficacy, and potential as a novel treatment for hormone-dependent cancers. These trials aim to determine the optimal dosing, administration, and patient populations that may benefit from this compound.
Used in Drug Resistance Research:
AZD3514 is utilized in research to explore its potential in overcoming resistance to existing hormone-targeted therapies. By understanding its mechanism of action and how it may interact with or overcome resistance mechanisms, researchers can develop more effective treatment strategies for patients with hormone-dependent cancers.
Used in Pharmaceutical Development:
AZD3514 is employed in the development of new pharmaceuticals targeting the androgen receptor. Its unique mechanism of action and potential to treat hormone receptor-positive cancers make it a valuable candidate for further research and development in the pharmaceutical industry.

Upstream product

• 1166819-39-1 6-[4-[4-[3-(4-acetylpiperazin-1-yl)propoxy]phenyl]piperidin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazine 
• 1166819-37-9 1-(4-(2-(4-(1-(3-(trifluoromethyl)-[1,2,4]triazolo[4,3-b]-pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)piperazin-1-yl)-ethanone 
• 40971-95-7 6-chloro-3-(trifluoromethyl)-[1,2,4]triazolo[4,3-b]pyridazine 
• 77279-24-4 tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate 
• 145943-75-5 3-(4-acetylpiperazin-1-yl)propan-1-ol 
• 1240300-04-2 tert-butyl 4-[2-[4-[1-[3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazine-1-carboxylate 
• 1240300-03-1 tert-butyl 4-[2-[4-[1-[3-(trifluoromethyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazine-1-carboxylate 
• 1240300-01-9 tert-butyl 4-[2-[4-(1-(benzyloxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]ethyl]piperazine-1-carboxylate 
• 1240299-99-3 benzyl 4-[4-[3-(4-acetylpiperazin-1-yl)propoxy]phenyl]-5,6-dihydropyridine-1(2H)-carboxylate 
• 1240300-02-0 tert-butyl 4-[2-[4-(piperidin-4-yl)phenoxy]ethyl]piperazine-1-carboxylate 
• 1240300-00-8 4-[4-[3-(4-acetylpiperazin-1-yl)propoxy]phenyl]piperidine 
• 19099-93-5 benzyl 4-oxo-1-piperidinecarboxylate 
• 1240300-05-3 6-[4-[4-[2-(piperazin-1-yl)ethoxy]phenyl]piperidin-1-yl]-3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazine 
• 75-36-5 acetyl chloride 

Downstream Products

• 1240299-36-8 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine maleate 
• 1240299-37-9 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine fumarate 
• 1240299-34-6 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3-(trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine napadisylate 

Relevant articles and documents

Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer

Removal of the basic piperazine nitrogen atom, introduction of a solubilising end group and partial reduction of the triazolopyridazine moiety in the previously-described lead androgen receptor downregulator 6-[4-(4-cyanobenzyl)piperazin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b] pyridazine (1) addressed hERG and physical property issues, and led to clinical candidate 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3- (trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine (12), designated AZD3514, that is being evaluated in a Phase I clinical trial in patients with castrate-resistant prostate cancer.

TRIAZOLO [4,3-B] PYRIDAZINE DERIVATIVES AND THEIR USES FOR PROSTATE CANCER

The invention concerns bicyclic compounds of Formula (I) wherein Formula (II), R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.