OTS193320
Based on 1 Customer Validation
OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX.
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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 : 99.11%
- CAS 番号: 2093401-33-1
- 分子式: C28H30ClN5O4
- 分子量:536.02
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保管条件:Powder -20°C, 3 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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Histone Methyltransferase 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
製品説明
IC50 & Target
[1]|
SUV39H2/KMT1B |
体外実験
OTS193320 (0.125-0.5 μM; 24 hours) has growth inhibitory effect on breast cancer cell lines. OTS193320 exhibits a high inhibitory effect against SUV39H2 enzymatic activity (IC50=22.2 nM) and a growth suppressive effect of SUV39H2-positive A549 lung cancer cells (IC50=0.38 μM)[1].
OTS193320 (0.5 μM; 48 hours) induces apoptosis in breast cancer cells[1].
OTS193320 (0.125-0.5 μM; 24 hours) causes attenuation of H3K9me3 levels in a dose-dependent manner[1].
OTS193320 sensitizes breast cancer cells to doxorubicin via attenuation of γ-H2AX. Combination of OTS193320 and doxorubicin (DOX) significantly attenuates cancer cell viability in vitro, compared to single agent treatment of either drug[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, SK-BR-3, ZR-75-1, T-47D, MDA-MB-231, BT-20 breast cancer cell lines
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Concentration:0-1 μM
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Incubation Time:72 hours
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Result:Had Growth inhibitory effect on MCF-7, SK-BR-3, ZR-75-1, T-47D, MDA-MB-231, and BT-20 breast cancer cell lines with IC50 values from 0.41 to 0.56 μM, respectively.
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Cell Line:MDA-MB-231 and BT-20 cells
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Concentration:0.5 μM
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Incubation Time:48 hours
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Result:Showed an increase in the number of cells at early- and late-stage apoptosis.
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Cell Line:MDA-MB-231 and BT-20 cells
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Concentration:0.125, 0.25, 0.5 μM
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Incubation Time:24 hours
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Result:Caused attenuation of H3K9me3 levels in a dose-dependent manner.
化学情報
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CAS 番号 2093401-33-1
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性状 Solid
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分子量 536.02
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分子式 C28H30ClN5O4
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Color Light yellow to yellow
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SMILES
O=[N+](C1=CC=C(CN[C@@H]2CC[C@H](NC3=CC4=NC(C5=CC(Cl)=C(OC)C=C5OC)=CN4C=C3)CC2)C=C1)[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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 62.5 mg/mL (116.60 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)
体内:
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: ≥ 6.25 mg/mL (11.66 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
In Vivo Dissolution Calculator
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 (272 KB)
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SDS (252 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 |
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| DMSO | 1 mM | 1.8656 mL | 9.3280 mL | 18.6560 mL | 46.6400 mL |
| 5 mM | 0.3731 mL | 1.8656 mL | 3.7312 mL | 9.3280 mL | |
| 10 mM | 0.1866 mL | 0.9328 mL | 1.8656 mL | 4.6640 mL | |
| 15 mM | 0.1244 mL | 0.6219 mL | 1.2437 mL | 3.1093 mL | |
| 20 mM | 0.0933 mL | 0.4664 mL | 0.9328 mL | 2.3320 mL | |
| 25 mM | 0.0746 mL | 0.3731 mL | 0.7462 mL | 1.8656 mL | |
| 30 mM | 0.0622 mL | 0.3109 mL | 0.6219 mL | 1.5547 mL | |
| 40 mM | 0.0466 mL | 0.2332 mL | 0.4664 mL | 1.1660 mL | |
| 50 mM | 0.0373 mL | 0.1866 mL | 0.3731 mL | 0.9328 mL | |
| 60 mM | 0.0311 mL | 0.1555 mL | 0.3109 mL | 0.7773 mL | |
| 80 mM | 0.0233 mL | 0.1166 mL | 0.2332 mL | 0.5830 mL | |
| 100 mM | 0.0187 mL | 0.0933 mL | 0.1866 mL | 0.4664 mL |
OTS193320 関連分類
HY-122182 関連分類
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