BI-847325CAS号： 1207293-36-4分子式： C29H28N4O2分子量： 464.56描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 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. |
| 纯度 |
98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
BI 847325；BI847325
|
| 外观 |
Powder
|
| 可溶性/溶解性 |
DMSO : 18 mg/mL (38.7 mM)
Ethanol : 1 mg/mL (2.15 mM) |
| 生物活性 | |
| 靶点 |
Aurora A (Human),Aurora B (Xenopus laevis),Aurora C (Human),MEK1,MEK2
|
| In vitro(体外研究) |
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(体内研究) |
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.
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| 参考文献 | |
| 参考文献 |
[1] Phadke MS, et al. Mol Cancer Ther. 2015, 14(6), 1354-1364. |
分子结构图
