2248003-60-1

2248003-60-1 structure

Name: AZD3229
Chemical Name: AZD3229
CAS Number: 2248003-60-1
Molecular Formula: C₂₄H₂₆FN₇O₃
Molecular Weight: 479.51
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK c-Kit
Create Date: 2019-02-11 10:03:22
Modify Date: 2024-01-07 12:02:31
AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

Name	AZD3229

Description	AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit Research Areas >> Cancer
Target	KIT[1].
In Vitro	AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM). AZD3229 Tosylate demonstrates potent single digit nM growth inhibition across a broad cell panel, with good margin to KDR-driven effects. Selectivity over KDR can be rationalised predominantly by the interaction of water molecules with the protein and ligand in the active site and its kinome selectivity is similar to the best of the approved GIST agents[1].
References	[1]. Kettle JG, et al. Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy) quinazolin-4-yl]amino} phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. J Med Chem. 2018 Oct 11;61(19):8797-8810.