Trilexium
Based on 1 Customer Validation
Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity.
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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: 99.70%
- CAS 番号: 1983180-82-0
- 分子式: C24H23FO6
- 分子量:426.43
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保管条件:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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生物活性
Trilexium shows activity against a broad range of cancer types. Of the 240 cell lines assessed in the Eurofin’s Oncopanel, 10 cell lines shows IC50 > 30 μM, of the remaining 230 cell lines, the average IC50 is 0.428 μM[1].
Trilexium (300 nM, 4 h) disrupts microtubule networks in Hela cells[1].
Trilexium (1-5 μM) leads to increased protein expression of p21, c-PARP, and c-Caspase 3 in HSJD-DIPG007 cells[2].
Trilexium (0-2 μM) restores H3K27 trimethylation and increases H3K27 acetylation in HSJD-DIPG007 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Trilexium (80 mg/kg, IV daily for 5 days) disrupts microtubules in vivo[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57/BL6 mice (n = 8 mice per group, subcutaneous mouse xenograft model of BRAF mutant (BRAFV600E) melanoma (A375))[1]
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Dosage:5 and 60 mg/kg
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Administration:IV (tail vein injection), daily for 15 days
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Result:Resulted in a tumour growth inhibition at 60 mg/kg. Significantly improved survival at 60 mg/kg.
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Animal Model:A375 xenografts mice[1].
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Dosage:80 mg/kg
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Administration:IV, daily for 5 days
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Result:Resulted in a loss of the long microtubule filaments in favour of shorter filaments and dispersed tubulin staining.
化学情報
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CAS 番号 1983180-82-0
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性状 Solid
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分子量 426.43
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分子式 C24H23FO6
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Color White to off-white
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SMILES
OC1=C(OC)C=C([C@H]2[C@@H](C3=CC(F)=C(C=C3)O)C4=CC=C(O)C(C)=C4OC2)C=C1OC
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別名
TRX-E-009-1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 300 mg/mL (703.52 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, 6 months; -20°C, 1 month (protect from light). 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 (protect from light). 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: ≥ 5 mg/mL (11.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Stevenson AJ, et al. Mechanism of action of the third generation benzopyrans and evaluation of their broad anti-cancer activity in vitro and in vivo. Sci Rep. 2018 Mar 23;8(1):5144. [Content Brief]
[2]. Ehteda A, et al. Microtubule-Targeting Combined with HDAC Inhibition Is a Novel Therapeutic Strategy for Diffuse Intrinsic Pontine Gliomas. Mol Cancer Ther. 2023 Dec 1;22(12):1413-1421. [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, 6 months; -20°C, 1 month (protect from light). 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 | 2.3451 mL | 11.7253 mL | 23.4505 mL | 58.6263 mL |
| 5 mM | 0.4690 mL | 2.3451 mL | 4.6901 mL | 11.7253 mL | |
| 10 mM | 0.2345 mL | 1.1725 mL | 2.3451 mL | 5.8626 mL | |
| 15 mM | 0.1563 mL | 0.7817 mL | 1.5634 mL | 3.9084 mL | |
| 20 mM | 0.1173 mL | 0.5863 mL | 1.1725 mL | 2.9313 mL | |
| 25 mM | 0.0938 mL | 0.4690 mL | 0.9380 mL | 2.3451 mL | |
| 30 mM | 0.0782 mL | 0.3908 mL | 0.7817 mL | 1.9542 mL | |
| 40 mM | 0.0586 mL | 0.2931 mL | 0.5863 mL | 1.4657 mL | |
| 50 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1725 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9771 mL | |
| 80 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 100 mM | 0.0235 mL | 0.1173 mL | 0.2345 mL | 0.5863 mL |