An inhibitor of c-Kit-driven cell proliferation
AZD 3229 is an inhibitor of c-Kit-driven cell proliferation.1 It selectively inhibits growth of c-Kit mutant (GI50s = 1-971 nM) and PDGFR mutant (GI50s = 1-22 nM) Ba/F3 cell lines over Ba/F3 cell lines expressing Tel-KDR/VEGFR2 (GI50 = 1,378 nM). AZD 3229 (20 mg/kg twice per day) induces tumor regression in a Ba/F3 mouse xenograft model and a mouse allograft model using Ba/F3 cells expressing KIT-exon 11 del/V654A, a common mutation in gastrointestinal stromal tumors (GIST).
1.Kettle, J.G., Anium, R., Barry, E., 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 tumorJ. Med. Chem.61(19)8797-8810(2018)
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