TAK-733

产品说明书

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Chemical Structure| 1035555-63-5 同义名 : -
CAS号 : 1035555-63-5
货号 : A118745
分子式 : C17H15F2IN4O4
纯度 : 99%+
分子量 : 504.23
MDL号 : MFCD24386349
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(69.41 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • MEK1

    MEK1, IC50:3.2 nM
描述 TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
A375 cells Cytotoxicity assay 72 h Cytotoxicity against human A375 cells after 72 hrs by MTS assay, EC50=3.1 nM 21310613
COLO205 cells Cytotoxicity assay 72 h Cytotoxicity against human COLO205 cells after 72 hrs by MTS assay, EC50=0.0021 μM 21310613
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.92mL

1.98mL

0.99mL

19.83mL

3.97mL

1.98mL
参考文献

[1]Micel LN, Tentler JJ, et al. Antitumor activity of the MEK inhibitor TAK-733 against melanoma cell lines and patient-derived tumor explants. Mol Cancer Ther. 2015 Feb;14(2):317-25.

[2]Dong Q, Dougan DR, et al. Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9.