1703793-34-3

Basic information

• Product Name: BLU-285
• Synonyms: BLU-285;Avapritinib;(1S)-1-(4-Fluorophenyl)-1-(2-{4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl}-5-pyrimidinyl)ethanamine
• CAS NO: 1703793-34-3
• Molecular Formula: C26H27FN10
• Molecular Weight: 498.5579832
• EINECS: -0
• Product Categories: API
• Mol File: 1703793-34-3.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Density: 1.42±0.1 g/cm3(Predicted)
• PKA: 6.96±0.10(Predicted)
• CAS DataBase Reference: BLU-285(CAS DataBase Reference)
• NIST Chemistry Reference: BLU-285(1703793-34-3)
• EPA Substance Registry System: BLU-285(1703793-34-3)

Safety Data

• Hazardous Substances Data: 1703793-34-3(Hazardous Substances Data)

Usage

Description

Avapritinib, also known as BLU-285, is a dual inhibitor of KIT receptor and platelet-derived growth factor receptor α (PDGFRα) tyrosine kinases with activating loop mutations. It is a potent, selective, and orally active medication that has demonstrated increased potency in cell lines expressing KIT and PDGFRα with activating loop mutations. Avapritinib is characterized by its high selectivity for KITD816V and PDGFRαD842V over a kinase panel at a concentration of 3 μM.

Uses

Used in Oncology:
Avapritinib is used as an anticancer agent for the treatment of tumors resulting from specific KIT and PDGFRα activating loop mutations. It has shown activity against a panel of KIT and PDGFRα loop mutants identified in patients with gastrointestinal stromal tumors (GISTs) and has demonstrated the ability to reduce tumor volume in various mouse models in a dose-dependent manner. Avapritinib is employed to inhibit the growth of cancer cell lines containing wild-type and mutant KIT and PDGFRα, particularly those with activating loop mutations, making it a promising therapeutic option for KITand PDGFRα-driven malignancies.