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Danusertib达鲁舍替

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品牌: yeasen
型号: 51101ES08
规格: 5mg
单价: 827.00元/支
发货期限: 自买家付款之日起 3 天内发货
所在地: 上海
有效期至: 长期有效
浏览次数: 3
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 产品信息

产品名称

产品编号

规格

储存

价格(元)

Danusertib达鲁舍替

51101ES08

5mg

-20 ºC

827.00 

Danusertib达鲁舍替

51101ES25

25mg

-20 ºC

2,677.00

产品描述                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                 

Danusertib又称PHA-739358,抑制Aurora kinase家族,作用于Aurora ABC,其IC50分别为137961 nM。除作用于Aurora kinase家族,Danusertib还抑制FGFR1c-AblRetTrk-A活性。Danusertib诱导p53依赖的核内增殖,当浓度超过50nM时,完全抑制培养的肿瘤细胞增殖并明显降低组蛋白H3磷酸化,而且在移植瘤模型中,Danusertib也表现出抗肿瘤作用,显著抑制肿瘤生长。

目前,Danusertib已进入Phase 2阶段。

【该产品仅用于科研实验,不能用于人体】

产品性质

中文别名(Chinese Synonym

达努塞替

英文别名(English Synonym

PHA-739358, PHA739358

化学名(Chemical Name

(R)-N-(5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-

4-(4-methylpiperazin-1-yl)benzamide

靶点(Target

Aurora kinase

CAS 号(CAS NO.

827318-97-8

分子式(Molecular Formula

C26H30N6O3

分子量(Molecular Weight

474.55

外观(Appearance

白色粉末

纯度(Purity

98%

溶解性(Solubility

溶于DMSO

结构式(Structure

 

运输与保存方法

粉末直接保存于-20 ºC有效期2年。易溶于DMSO。建议分装后-20ºC光保存,避免反复冻存,至少可存放6个月。

注意事项

1为了您的安全和健康,请穿实验服并戴一次性手套操作。

2)粉末溶解前请先短暂离心,以保证产品全在管底。

3)本产品仅用于科研用途,禁止用于人身上。


使用浓度

具体使用浓度请参考相关文献,并根据自身实验条件(如实验目的,细胞种类,培养特性等)进行摸索和优化。

相关实验(数据来自于公开发表的文献,仅供参考)

(一)细胞实验

1)使用不同浓度的Danusertib (PHA-7393580.01-10μM)孵育HeLa细胞1hWestern blot检测磷酸化Aurora AAurora B介导的组蛋白H3磷酸化,结果显示,随Danusertib浓度增加,其抑制作用越来越显著。另外,用分别0.51μM Danusertib处理HCT-116细胞24h,发现p53蛋白水平提高,而且p21蛋白水平也相应提高。[1]

2)为研究Danusertib (PHA-739358)对肿瘤细胞的作用,使用550500nM Danusertib分别处理Huh-7HepG2细胞,当浓度超过50nM时,Danusertib表现出明显的抗增殖作用,肿瘤细胞几乎停止生长。[2]

(二)动物实验

1)为检测Danusertib (PHA-739358的抗肿瘤活性,建立HL-60移植瘤小鼠模型,静脉注射30 mg/kg/day持续5天,肿瘤生长抑制率(TGI)达到98%,在治疗结束1周后达到完全的抑制,肿瘤完全收缩[1]

2)每天2次用15mg/kg Danusertib (PHA-739358)处理Huh-7HepG2移植瘤模型,分别处理36912天,发现,Danusertib 有效抑制Huh-7HepG2肿瘤生长。从第3天开始,Huh-7肿瘤生长就被明显抑制。[2]

参考文献

[1] Patrizia Carpinelli, et al. PHA-739358, a potent inhibitor of aurora kinases with a selecyive target inhibiton profile relevant to cancer. Mol Cancer Ther 6(12 Pt 1): 3158-3168(2007).

[2] Daniel Benten, et al. Aurora Kinase Inhibitor PHA-739358 Suppresses Growth of Hepatocellular Carcinoma In Vitro and in a Xenograft Mouse Model. Neoplasia 11(9): 934-944(2009).

 

生物帮站内所有产品仅限于生命科学实验室科学研究使用,不得用于临床诊断及药物治疗。

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