AZD3229

Modify Date: 2024-01-07 12:02:31

AZD3229 Structure
AZD3229 structure
Common Name AZD3229
CAS Number 2248003-60-1 Molecular Weight 479.51
Density N/A Boiling Point N/A
Molecular Formula C24H26FN7O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AZD3229


AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

 Names

Name AZD3229

 AZD3229 Biological Activity

Description AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
Related Catalog
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.

 Chemical & Physical Properties

Molecular Formula C24H26FN7O3
Molecular Weight 479.51
Storage condition 2-8℃