TAK1/MAP4K2 inhibitor 1
Based on 1 publication(s) in Google Scholar
TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 1315330-11-0
- Formula: C29H31F3N6O2
- Molecular Weight:552.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) TAK1/MAP4K2 inhibitor 1
MoreAll MAP4K Isoforms
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Biological Activity
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TAK1 41.1 nM (IC50) |
MAP4K2 18.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
>10 μM
Compound: 5
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Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
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[PMID: 25075558] |
| BaF3 | IC50 |
0.02 μM
Compound: 5
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Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
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[PMID: 25075558] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1315330-11-0
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Appearance Solid
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Molecular Weight 552.59
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Formula C29H31F3N6O2
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Color White to light yellow
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SMILES
CC(N1)=CC2=C1N=CN=C2OC3=C(C)C=CC(C(NC4=CC=C(CN5CCN(CC)CC5)C(C(F)(F)F)=C4)=O)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Korean J Physiol Pharmacol
The WNT/Ca2+ pathway promotes atrial natriuretic peptide secretion by activating protein kinase C/transforming growth factor-β activated kinase 1/activating transcription factor 2 signaling in isolated beating rat atria. [Abstract]2022 Nov 1;26(6):469-478. PMID: 36302622
Solvent & Solubility
DMSO : 50 mg/mL (90.48 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (4.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (4.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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 | 1.8097 mL | 9.0483 mL | 18.0966 mL | 45.2415 mL |
| 5 mM | 0.3619 mL | 1.8097 mL | 3.6193 mL | 9.0483 mL | |
| 10 mM | 0.1810 mL | 0.9048 mL | 1.8097 mL | 4.5241 mL | |
| 15 mM | 0.1206 mL | 0.6032 mL | 1.2064 mL | 3.0161 mL | |
| 20 mM | 0.0905 mL | 0.4524 mL | 0.9048 mL | 2.2621 mL | |
| 25 mM | 0.0724 mL | 0.3619 mL | 0.7239 mL | 1.8097 mL | |
| 30 mM | 0.0603 mL | 0.3016 mL | 0.6032 mL | 1.5080 mL | |
| 40 mM | 0.0452 mL | 0.2262 mL | 0.4524 mL | 1.1310 mL | |
| 50 mM | 0.0362 mL | 0.1810 mL | 0.3619 mL | 0.9048 mL | |
| 60 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7540 mL | |
| 80 mM | 0.0226 mL | 0.1131 mL | 0.2262 mL | 0.5655 mL |