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
• Article Data: 2

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

General Description

AZD3514 is a selective androgen receptor down-regulator (SARD) that has shown promise in the treatment of hormone receptor-positive breast cancer and other hormone-dependent cancers. It works by targeting the androgen receptor, which is a key driver of tumor growth in some hormone-dependent cancers. AZD3514 has been shown to inhibit the growth of cancer cells in preclinical studies and is currently being evaluated in clinical trials. It has the potential to provide a novel treatment option for patients with hormone receptor-positive cancers and may offer a new mechanism of action for overcoming resistance to existing hormone-targeted therapies.

Upstream product

• 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 
• 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 
• 19099-93-5 benzyl 4-oxo-1-piperidinecarboxylate 
• 1240300-00-8 4-[4-[3-(4-acetylpiperazin-1-yl)propoxy]phenyl]piperidine 
• 1240300-02-0 tert-butyl 4-[2-[4-(piperidin-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 
• 1240300-01-9 tert-butyl 4-[2-[4-(1-(benzyloxycarbonyl)-1,2,3,6-tetrahydropyridin-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 
• 1240300-04-2 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 
• 145943-75-5 3-(4-acetylpiperazin-1-yl)propan-1-ol 
• 77279-24-4 tert-butyl 4-(2-hydroxyethyl)piperazine-1-carboxylate 

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.