aladdin 阿拉丁 B413849 BI-847325 1207293-36-4 98%

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 

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