1672665-49-4

Basic information

• Product Name: PT-2385
• Synonyms: PT-2385
• CAS NO: 1672665-49-4
• Molecular Formula: C17H12F3NO4S
• Molecular Weight: 383.3416896
• Mol File: 1672665-49-4.mol
• Article Data: 7

Chemical Properties

• Boiling Point: 524.7±50.0 °C(Predicted)
• Appearance: /
• Density: 1.57±0.1 g/cm3(Predicted)
• Storage Temp.: Sealed in dry,Store in freezer, under -20°C
• PKA: 11.28±0.40(Predicted)
• CAS DataBase Reference: PT-2385(CAS DataBase Reference)
• NIST Chemistry Reference: PT-2385(1672665-49-4)
• EPA Substance Registry System: PT-2385(1672665-49-4)

Safety Data

• Hazardous Substances Data: 1672665-49-4(Hazardous Substances Data)

Usage

Uses

PT2385 is a HIF-2α antagonist with EC50 of 27 nM in the luciferase assay, with no apparent off-target effects.

Upstream product

• 136191-16-7 4-Fluoro-7-hydroxy-indan-1-one 
• 1073-72-9 4-hydroxythioanisole 
• 67868-84-2 5-methylthio-2-hydroxybenzaldehyde 
• 1672665-69-8 3-fluoro-5-((7-(methylthio)-1-oxo-2,3-dihydro-1H-inden-4-yl)oxy)benzonitrile 
• 473923-95-4 3-fluoro-5-hydroxy-benzonitrile 
• 433939-27-6 3-bromo-5-fluorophenol 

Relevant articles and documents

Method for preparing HIF-2 alpha inhibitor PT2385

The invention relates to a preparation method of HIF-2 alpha inhibitor PT2385. To the method, difluorobenzene is taken as a raw material, and reacted with 3 - chloropropionyl chloride to generate an intermediate II which reacts with sodium methoxide to generate an intermediate III which is subsequently oxidized. The intermediate VII is obtained through an oxidation reaction, and the intermediate VIII is obtained by reaction with n-butylamine to obtain compound IX which is subjected to fluorination reaction and hydrolysis to obtain intermediate X which is finally subjected to asymmetric reduction reaction to obtain final product PT2385. Compared with the existing synthetic method, the process route provided by the invention has the obvious advantages of cheap and easily available raw materials, simple operation, few reaction steps, high total yield of 47.6%, avoidance of multi-step high-temperature reaction and easiness in industrial production. .

COMBINATION THERAPY OF A HIF-2-ALPHA INHIBITOR AND AN IMMUNOTHERAPEUTIC AGENT AND USES THEREOF

The present invention provides methods and pharmaceutical compositions for treating proliferative disorders. The method involves step of administering to said subject a HIF-2alpha inhibitor and an immunotherapeutic agent.

HIF-2-ALPHA INHIBITOR POLYMORPHS

Chemical compounds that modulate HIF-2α activity, their polymorphs, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with HIF-2α, are described herein.