TMX-4116
Based on 1 Customer Validation
TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.76%
- CAS 番号: 2766385-56-0
- 分子式: C17H19N5O4S
- 分子量:389.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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CK1α |
TMX-4116 (compound 16; 1 μM; 4 h) shows a high degradation preference for CK1α in MOLT4 cells[1].
TMX-4116 (250 nM, 4 h) induces primary target degradation of CK1α, while no downregulation of PDE6D, IKZF1, and IKZF3 in MOLT4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT4 cells
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Concentration:1 μM
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Incubation Time:4 hours
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Result:Showed a high degradation preference for CK1α.
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Cell Line:MOLT4, Jurkat, and MM.1S cells
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Concentration:0 nM, 40 nM, 200 nM, 1 μM
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Incubation Time:4 hours
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Result:Showed a high degradation preference for CK1α with the DC50 value less than 200 nM in MOLT4, Jurkat, and MM.1S cells.
化学情報
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CAS 番号 2766385-56-0
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性状 Solid
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分子量 389.43
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分子式 C17H19N5O4S
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Color Off-white to gray
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SMILES
O=C(C(N1N=NC(C2=CSC(C(N3CCCC3)=O)=C2OC)=C1)CC4)NC4=O
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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 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (256.79 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5679 mL | 12.8393 mL | 25.6786 mL | 64.1964 mL |
| 5 mM | 0.5136 mL | 2.5679 mL | 5.1357 mL | 12.8393 mL | |
| 10 mM | 0.2568 mL | 1.2839 mL | 2.5679 mL | 6.4196 mL | |
| 15 mM | 0.1712 mL | 0.8560 mL | 1.7119 mL | 4.2798 mL | |
| 20 mM | 0.1284 mL | 0.6420 mL | 1.2839 mL | 3.2098 mL | |
| 25 mM | 0.1027 mL | 0.5136 mL | 1.0271 mL | 2.5679 mL | |
| 30 mM | 0.0856 mL | 0.4280 mL | 0.8560 mL | 2.1399 mL | |
| 40 mM | 0.0642 mL | 0.3210 mL | 0.6420 mL | 1.6049 mL | |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5136 mL | 1.2839 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4280 mL | 1.0699 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3210 mL | 0.8025 mL | |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6420 mL |
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