产品属性：
产品名称 | 规格 | CAS号 | 型号 |
BI-847325 | 5mg 25mg 100mg | 1207293-36-4 | EY-Y0165442 |
Cas No.1207293-36-4
别名
化学名 (Z)-3-(3-(((4-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide
分子式 C29H28N4O2
分子量 464.56
溶解度 DMF: 16 mg/ml,DMF:PBS(pH 7.2)(1:6): 0.14 mg/ml,DMSO: 5 mg/ml,Ethanol: 0.3 mg/ml
储存条件 Store at -20°C
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
产品描述：
The RAS-dependent MAP kinase signaling pathway is important in the regulation of cell survival and proliferation. It is hard to design direct inhibitors of RAS proteins. MEK is a downstream kinase of MAP kinase [1]. MEK is a ERK kinase [3].
In cells treated with BI 847325, based on levels of phospho-histone H3 (pHH3) and phospho-ERK (pERK), EC50 values were determined. To KRAS-and-PI3Kα-mutant NCI-H460 cells, the EC50 value was 44 nM. To BRAF-mutant A375 cells, the EC50 value was 37 nM. In a panel of 240 cell lines from diverse tissues with diverse genetic background, BI 847325 produced a potent inhibition of cell proliferation with a gm GI50 value of 28 nM. In a subset of cell lines, BI 847325 induced cell death. These in vitro potency correlated with mutations in BRAF or RAS, significantly [1].
In nude mouse xenograft models of cutaneous melanoma (A375, mutant BRAF) and NSCLC (Calu-6, mutant KRAS), BI 847325 at a daily oral dose of 10 mg/kg produced complete inhibition of tumor growth. In animals with A375 tumors, treatment with BI 847325 significantly reduced levels of both pHH3 and pERK in the tumors compared to controls [1].
References:
[1]. Sini P, Gürtler U, Zahn SK, et al. Pharmacological characterization of BI 847325, a dual inhibitor of MEK and Aurora kinases. Cancer Research, 2012, 72(8 Supplement): 1919-1919.
[2]. Hideshima T, Chauhan D, Richardson P, et al. NF-κB as a therapeutic target in multiple myeloma. Journal of Biological Chemistry, 2002, 277(19): 16639-16647.
[3]. Rommel C, Clarke BA, Zimmermann S, et al. Differentiation stage-specific inhibition of the Raf-MEK-ERK pathway by Akt. Science, 1999, 286(5445): 1738-1741..
关键字： 1207293-36-4;C29H28N4O2;BI-847325;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业，公司自成立以来，秉承""全心全意服务于科研工作者""的企业理念，立足生物科技领域，运用生物技术和科研试剂，发展现代生物科技，为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品，服务生物科技领域的科学研究人员。
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