AZD 3229

c-Kit驱动细胞增殖的抑制剂；选择性抑制c-Kit突变体(GI50s=1-971nM)和PDGFR突变体(GI50s=1-22nM)Ba/F3细胞系的生长，优于表达Tel-KDR/VEGFR2(GI50=1,378nM)的Ba/F3细胞系；以每天20mg/kg的剂量在Ba/F3小鼠异种移植模型中诱导肿瘤消退；以每天两次20mg/kg的剂量在表达KIT-外显子11del/V654A的Ba/F3细胞的小鼠同种异体移植模型中诱导肿瘤消退。An inhibitor of c-Kit-driven cell proliferation; 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); induces tumor regression in a Ba/F3 mouse xenograft model at 20 mg/kg per day; induces tumor regression in a mouse allograft model using Ba/F3 cells expressing KIT-exon 11 del/V654A at 20 mg/kg twice per day.