WH244
Based on 1 Customer Validation
WH244 is a BCL-xL and BCL-2 PROTAC degrader with DC50 values of 0.6 nM and 7.4 nM, and Kd values of 6.14 nM and 3.1 nM, respectively. WH244 kills cancer cells dependent on BCL-xL and BCL-2 for survival. WH244 is applicable to relevant research on leukemia.
(Pink: Bcl-2 and Bcl-xL ligand (HY-161415); Blue: VHL ligand (HY-112078); Black: linker (HY-161444)).
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 : 99.82%
- CAS 番号: 2941088-96-4
- 分子式: C83H105ClF3N13O11S4
- 分子量:1681.51
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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
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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs 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]|
Bcl-xL 0.6 nM (DC50) |
Bcl-2 7.4 nM (DC50) |
体外実験
WH244 (0-100 nM; 1-24 h) potently degrades BCL-xL (DC50 = 0.6 nM) and BCL-2 (DC50 = 7.4 nM) in Jurkat cells in a time-dependent, reversible, VHL-dependent and UPS-dependent manner[1].
WH244 (0.001-1 μM; 72 h) reduces the viability of Jurkat cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:Jurkat cells
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Concentration:0.001, 0.01, 0.1, and 1 μM
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Incubation Time:72 h
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Result:Exhibited enhanced potency in reducing Jurkat cell viability.
化学情報
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CAS 番号 2941088-96-4
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性状 Solid
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分子量 1681.51
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分子式 C83H105ClF3N13O11S4
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Color White to off-white
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SMILES
CC1=C(C2=CC=C([C@@H](NC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CN4CCN(CC(N5CCN(C[C@]6(C)CCC(C7=CC=C(Cl)C=C7)=C(CN8CCN(C9=CC=C(C(NS(C%10=CC(S(C(F)(F)F)(=O)=O)=C(N[C@@H](CSC%11=CC=CC=C%11)CCN%12C[C@@H]%13OC[C@H]%12C%13)C=C%10)(=O)=O)=O)C=C9)CC8)C6)CC5)=O)CC4)=O)C(C)(C)C)=O)=O)C)C=C2)SC=N1
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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
体外:
DMSO : 100 mg/mL (59.47 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. 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: ≥ 2.5 mg/mL (1.49 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.
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 (270 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 0.5947 mL | 2.9735 mL | 5.9470 mL | 14.8676 mL |
| 5 mM | 0.1189 mL | 0.5947 mL | 1.1894 mL | 2.9735 mL | |
| 10 mM | 0.0595 mL | 0.2974 mL | 0.5947 mL | 1.4868 mL | |
| 15 mM | 0.0396 mL | 0.1982 mL | 0.3965 mL | 0.9912 mL | |
| 20 mM | 0.0297 mL | 0.1487 mL | 0.2974 mL | 0.7434 mL | |
| 25 mM | 0.0238 mL | 0.1189 mL | 0.2379 mL | 0.5947 mL | |
| 30 mM | 0.0198 mL | 0.0991 mL | 0.1982 mL | 0.4956 mL | |
| 40 mM | 0.0149 mL | 0.0743 mL | 0.1487 mL | 0.3717 mL | |
| 50 mM | 0.0119 mL | 0.0595 mL | 0.1189 mL | 0.2974 mL |
WH244 関連分類
HY-161410 関連分類
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