产品信息
抗原名称
Abl (Q252H),Abl (E255K),Abl (M351T),Abl,Abl (H396P),,
商品描述
GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.
分子量
724.77
纯度
>98%
可溶性
DMSO 100 mg/mL (137.97 mM)
Water 100 mg/mL (137.97 mM)
Water 100 mg/mL (137.97 mM)
外观
Powder
In vitro(体外研究)
GZD824 potently inhibits the growth of Ba/F3 cells expressing wildtype Bcr-Abl with IC50 of 1.0 nM. Highly consistent with biochemical kinase inhibition and tight protein binding affinity, GZD824 also strongly inhibits the proliferation of Ba/F3 cells expressing Bcr-AblT315I mutant and 14 other resistance-relevant Bcr-Abl mutants. In addition, GZD824 efficiently suppresses the activation of Bcr-Abl as well as downstream Crkl and STAT5 in a concentration-dependent manner in K562 CML cells.
In vivo(体内研究)
GZD824, at doses of 5 and 10 mg/kg/day, dose-dependently inhibits the tumor growth in the K562 tumor xenograft and the Ku812 xenograft model without mortality or significant body loss. Besides, GZD824 (20 mg/kg/day) suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-AblWT and Bcr-AblT315I.
背景
别名
GZD-824; GZD 824,Benzamide
分子式
C29H27F3N6O.2CH4O3S
CAS号
1421783-64-3
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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