TAK-733
Based on 6 publication(s) in Google Scholar
TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.79%
- CAS 番号: 1035555-63-5
- 分子式: C17H15F2IN4O4
- 分子量:504.23
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 TAK-733
More- Exp Mol Med. 2018 Apr 20;50(4):37. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- J Invest Dermatol. 2022 Mar;142(3 Pt A):613-623.e7. [Abstract]
- Oncogenesis. 2025 Mar 1;14(1):4. [Abstract]
- ACS Comb Sci. 2019 Dec 9;21(12):805-816. [Abstract]
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MEK アイソフォーム固有の製品をすべて表示
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生物活性
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MEK 3.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | EC50 |
3.1 nM
Compound: 17, TAK-733
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Cytotoxicity against human A375 cells after 72 hrs by MTS assay
Cytotoxicity against human A375 cells after 72 hrs by MTS assay
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[PMID: 21310613] |
| COLO 205 | EC50 |
2.1 nM
Compound: 17, TAK-733
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Cytotoxicity against human COLO205 cells after 72 hrs by MTS assay
Cytotoxicity against human COLO205 cells after 72 hrs by MTS assay
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[PMID: 21310613] |
| COLO 205 | IC50 |
6.92 nM
Compound: TAK-733
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Inhibition of MEK1 in human COLO205 cells
Inhibition of MEK1 in human COLO205 cells
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[PMID: 24755426] |
TAK-733 exhibits potent enzymatic and cell activity with an IC50 of 3.2 nM against constitutively active MEK enzyme and an EC50 of 1.9 nM against ERK phosphorylation in cells. TAK-733 does not inhibit any other kinases, receptors or ion channels that are tested with inhibitor concentrations up to 10 μM. TAK-733 is found to bind plasma protein moderately (ca. 97% for human and 96% for mouse), and exhibits high permeability and high microsomal stability across species. It does not inhibit P450s up to 30 μM[1]. TAK-733 demonstrates broad activity in most melanoma cell lines with relative resistance observed at IC50 >0.1 μM in vitro. Thirty-four melanoma cell lines are exposed in vitro to increasing concentrations of TAK-733 for 72 hours. Of the 34 cell lines, 27 are BRAFV600E mutant and 7 are wild-type. SRB proliferation assays are performed and the resulting IC50 concentrations allowed stratification of cell lines into three categories: relatively resistant, intermediate, and highly sensitive. Relatively resistant and highly sensitive lines are assigned based on an IC50 that differ by at least 10 fold[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1035555-63-5
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性状 Solid
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分子量 504.23
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分子式 C17H15F2IN4O4
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Color White to light yellow
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SMILES
O=C1C(C(NC2=CC=C(I)C=C2F)=C(F)C(N3C)=O)=C3N=CN1C[C@@H](O)CO
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Exp Mol Med
TAK-733 inhibits inflammatory neointimal formation by suppressing proliferation, migration, and inflammation in vitro and in vivo. [Abstract]2018 Apr 20;50(4):37. PMID: 29674718
TAK-733 purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2018 Apr 20;50(4):37. [Abstract]
TAK-733 attenuates the Ang II-induced increases in cyclin D1 and PCNA protein expression.
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
J Invest Dermatol
Combined Cyclin-Dependent Kinase Inhibition Overcomes MAPK/Extracellular Signal-Regulated Kinase Kinase Inhibitor Resistance in Plexiform Neurofibroma of Neurofibromatosis Type I. [Abstract]2022 Mar;142(3 Pt A):613-623.e7. PMID: 34534577 -
Oncogenesis
STAG2 expression imparts distinct therapeutic vulnerabilities in muscle-invasive bladder cancer cells. [Abstract]2025 Mar 1;14(1):4. PMID: 40025053 -
ACS Comb Sci
Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]2019 Dec 9;21(12):805-816. PMID: 31689077
溶剤 & 溶解度
DMSO : 100 mg/mL (198.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
The cutaneous melanoma cell lines in logarithmic growth phase are transferred to 96 well flat bottom plates with lids. One hundred μL cell suspensions containing 2000-3000 viable cells are plated into each well and incubated overnight prior to exposure with increasing concentrations of TAK-733 (10, 20, 30, 40, 50, 60, 70, 80, 90, and 100 nM) for 72 hours. Post drug administration, media is removed and cells are fixed with cold 10% trichloroacetic acid for 30 min. at 4°C. Cells are then washed with water and stained with 0.4% SRB for 30 min at room temperature, washed again with 1% acetic acid, followed by stain solubilization with 10 mM tris at room temperature. The absorbance at 565 nm is measured on a plate reader. Cell proliferation curves are derived from the raw absorbance (OD) data. Statistical analyses and graphical representation of data are using GraphPad Prism version 5.00[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Five to six-week-old female athymic nude mice are used. A375 human melanoma xenograft tumors are generated by harvesting cells from mid-log phase cultures using Trypsin-EDTA. Approximately 5×106 cells suspended in Hanks’ balanced salt solution (HBSS) are injected sc into the right flank of 6-8-week-old mice. Oral administration of TAK-733 (1 mg/kg or 10 mg/kg) is initiated when tumors in all mice in each experiment range in size from 100 to 200 mm3 for antitumor efficacy studies and from 300 to 500 mm3 for pharmacodynamic (PD) studies[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (396 KB)
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- Français - FR (396 KB)
- Deutsch - DE (396 KB)
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- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Dong Q, 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. [Content Brief]
[2]. Micel LN, 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9832 mL | 9.9161 mL | 19.8322 mL | 49.5805 mL |
| 5 mM | 0.3966 mL | 1.9832 mL | 3.9664 mL | 9.9161 mL | |
| 10 mM | 0.1983 mL | 0.9916 mL | 1.9832 mL | 4.9581 mL | |
| 15 mM | 0.1322 mL | 0.6611 mL | 1.3221 mL | 3.3054 mL | |
| 20 mM | 0.0992 mL | 0.4958 mL | 0.9916 mL | 2.4790 mL | |
| 25 mM | 0.0793 mL | 0.3966 mL | 0.7933 mL | 1.9832 mL | |
| 30 mM | 0.0661 mL | 0.3305 mL | 0.6611 mL | 1.6527 mL | |
| 40 mM | 0.0496 mL | 0.2479 mL | 0.4958 mL | 1.2395 mL | |
| 50 mM | 0.0397 mL | 0.1983 mL | 0.3966 mL | 0.9916 mL | |
| 60 mM | 0.0331 mL | 0.1653 mL | 0.3305 mL | 0.8263 mL | |
| 80 mM | 0.0248 mL | 0.1240 mL | 0.2479 mL | 0.6198 mL | |
| 100 mM | 0.0198 mL | 0.0992 mL | 0.1983 mL | 0.4958 mL |
TAK-733 関連分類
HY-13449 関連分類
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