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CAS No.: 1035555-63-5

TAK-733 Catalog No. CSN16108

Synonyms: TAK-733

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.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00948467	Advanced Non-hematologic Malig... more >>nancies Advanced Metastatic Melanoma Collapse <<	Phase 1	Completed	-	United States, Michigan ... more >> Wayne State University Karmanos Cancer Institute Detriot, Michigan, United States, 48201 United States, New York Roswell Park Cancer Institute Buffalo, New York, United States, 14263 Collapse <<
NCT01613261	Advanced Nonhematologic Malign... more >>ancies Collapse <<	Phase 1	Withdrawn	November 2015	United States, Texas ... more >> South Texas Accelerated Research Therapeutics (START) San Antonio, Texas, United States, 78229 Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9832 mL
- 9.9162 mL
- 19.8323 mL
- 5 mM
- 0.3966 mL
- 1.9832 mL
- 3.9665 mL
- 10 mM
- 0.1983 mL
- 0.9916 mL
- 1.9832 mL

技术信息

CAS号

1035555-63-5

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H15F2IN4O4

运输

蓝冰

分子量

504.23

别名

TAK-733

溶解度

DMSO	101.0 mg/mL (200.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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