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BI-847325

CAS号

1207293-36-4

分子式

C29H28N4O2

主要靶点

Apoptosis|Aurora Kinase|MEK

仅限科研使用

Cat No : CM03077

Print datasheet

Synonyms

Apoptosis|AuroraKinase|Aurora Kinase|Aurora A (Human)|Aurora C (Human)|Aurora B (Xenopus laevis)|BI 847325|BI847325|BI-847325|inhibit|Inhibitor|Mitogen-activated protein kinase kinase|MEK2|MEK1|MEK|MAPKK|MAP2K

验证数据展示

  • CAS No.: 1207293-36-4

    BI-847325
    CAS#: 1207293-36-4

产品信息

CAS号 1207293-36-4
分子式 C29H28N4O2
主要靶点 Apoptosis|Aurora Kinase|MEK
主要通路 细胞周期|表观遗传|凋亡|MAPK 信号通路
分子量 464.56
纯度 97.54%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Apoptosis|AuroraKinase|Aurora Kinase|Aurora A (Human)|Aurora C (Human)|Aurora B (Xenopus laevis)|BI 847325|BI847325|BI-847325|inhibit|Inhibitor|Mitogen-activated protein kinase kinase|MEK2|MEK1|MEK|MAPKK|MAP2K

靶点活性

Aurora kinase:15 nM|MEK:4nM

体内活性

在携带1205Lu和1205LuR异种移植瘤的小鼠中，BI-847325（75 mg/kg，口服）明显抑制了肿瘤的生长，而且没有显著改变体重。[1]

体外活性

BI-847325 在BRAF突变和对vemurafenib耐药的黑色素瘤细胞上显示出生长抑制效果，其IC50值在0.3 nM到2 μM范围内，并且在六个BRAF突变的黑色素瘤细胞系中阻止了集落形成。BI-847325 还通过减少Mcl-1表达来诱导凋亡。[1]

溶解度

H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:18 mg/mL (38.75 mM);Ethanol:1 mg/mL (2.15 mM)

细胞实验

Cells are plated at a density of 2.5 × 103 cells per 100 μL and left to grow overnight before being treated with increasing concentrations of BI-847325 for 72 hours. The metabolic activity is determined using Alamar blue reagent as per the manufacturer's protocol.(Only for Reference)

参考文献

1.Phadke MS, et al. Mol Cancer Ther. 2015, 14(6), 1354-1364.

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