中文名：BI-847325
英文名：BI-847325
纯度：≥98%
货号：B413849
Cas号：1207293-36-4
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
BI-847325 is an orally bioavailable, and selective dualMEK/Aurora kinaseinhibitor withIC50of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
Targets
Aurora B (Xenopus laevis) ; MEK2 ; Aurora C (Human) ; Aurora A (Human) ; MEK1 3 nM; 4 nM; 15 nM; 25 nM; 25 nM
In vitro
BI-847325 shows growth-inhibitory effects on BRAF-mutant and vemurafenib-resistant melanoma cells with IC50 ranging from 0.3 nM to 2 μM, and prevents colony formation in six BRAF-mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression.
In vivo
In mice bearing 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) causes significant tumor suppression without significant alteration in the body weights.
Cell Research(from reference)
Cell lines：M229, M229R, A375, A375R, WM793, WM793R, 1205Lu, 1205LuR, M249, M249R, WM164, WM164R, WM39 and RPMI17951 cells
Concentrations：30 μM
Incubation Time：72 h
查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/B413849.html
关键字： NSC799360 ; NSC-799360 ; (Z)-3-(3-((4-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide ; 2-Propynamide, 3-((3Z)-3-(((4-((dimethylamino)methyl)phenyl)amino)phenylmethylene)-2,3-dihydro-2-oxo-1H-indol-6-yl)-N-ethy
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