GZD824 Dimesylate,1421783-64-3

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YZ剂描述：

产品名称：GZD824 Dimesylate

产品别名：GZD-824; GZD 824,Benzamide

英文别名：GZD-824;GZD 824;Benzamide

靶点：Abl (Q252H) ，Abl (E255K) ，Abl (M351T) ，Abl ，Abl (H396P) ，,

CAS：1421783-64-3

纯度：>98%

外观：Powder

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

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.

溶解性：DMSO100 mg/mL (137.97 mM)
Water100 mg/mL (137.97 mM)

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.

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.

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