產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 25mg
CAS	1421783-64-3
別名
化學(xué)名	3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide dimethanesulfonate
分子式	C29H27F3N6O.2CH4O3S
分子量	724.77
溶解度	≥ 36.25mg/mL in DMSO
儲存條件	4°C, away from moisture and light
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

GZD824 is an orally bioavailable inhibitor of Bcr-Abl with IC50 values of 0.34 and 0.68 nM for Bcr-AblWT and Bcr-AblT315I, respectively [1].

Bcr-Abl is a fused protein that interacts with the interleukin-3 receptorβ(c) subunit and has tyrosine kinase activity. Abl activates cell cycle-related proteins and enzymes and increases cell division. Bcr-Abl inhibits DNA repair and causes genomic instability.

GZD824 is an orally bioavailable Bcr-Abl inhibitor. GZD824 exhibited high affinity with Kd values of 0.32 and 0.71 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GZD824 inhibited Bcr-Abl with IC50 values of 0.34, 0.68, 0.27, 0.71, 0.15, 0.35, 0.29 and 0.35 nM for Bcr-AblWT, Bcr-AblT315I, Bcr-AblE255K, Bcr-AblG250E, Bcr-AblQ252H, Bcr-AblH396P, Bcr-AblM351T and Bcr-AblY253F, respectively. In a competitive binding assay, GZD824 bound to the ATP-binding sites of native Abl with Kd values of 0.32 and 0.34 nM for non-phosphorylated and phosphorylated Abl. In stably transformed Ba/F3 cells, GZD824 potently inhibited cells growth with IC50 values of 1.0 and 7.1 nM for Bcr-AblWT and Bcr-AblT315I expressed cells, respectively [1].

In mouse xenograft tumor models, GZD824 inhibited tumor growth. In mice bearing an allograft leukemia model, GZD824 significantly increased survival [1].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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