DB-0646
Based on 1 Customer Validation
DB-0646 is a multi-target PROTAC degrader that degrades over 125 distinct kinases in various cell lines, with its degradation process dependent on the activity of p97. DB-0646 induces ubiquitination and degradation of GCK, BUB1 and YES1.
(Pink: GCK and BUB1 and YES1 ligand (HY-176367); Blue: Cereblon ligand (HY-10984); Black: linker).
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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: 98.0%
- CAS 番号: 2769753-59-3
- 分子式: C52H51F3N14O7
- 分子量:1041.05
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
生物活性
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GCK/MAP4K2 |
Yes |
BUB1 |
Cereblon |
DB-0646 (1 μM; 5 h) induces significant degradation of multiple kinases including CSK, FER, and LIMK2, with the highest number of degraded kinase targets observed in MOLT-4 cells, followed by KELLY and HEK293T cells[1].
DB-0646 (1 μM; 5 h) degradation of kinases including CSK, FER, and LIMK2 in MOLT-4 cells is p97-dependent, as co-treatment with p97 inhibitor CB-5083 reverses the degradation effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2769753-59-3
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性状 Solid
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分子量 1041.05
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分子式 C52H51F3N14O7
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Color Off-white to light yellow
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SMILES
O=C(N1C2CCC(NC2=O)=O)C3=C(OCCCCCN4N=NC(CN5CCN(C6=NC=C(NC7=NC=C8C(N(C)C(N(C9=CC(NC(C%10=CC=CC(C(F)(F)F)=C%10)=O)=CC=C9C)C8)=O)=N7)C=C6)CC5)=C4)C=CC=C3C1=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
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
DMSO : 50 mg/mL (48.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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 (stored under nitrogen). 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 (stored under nitrogen). 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: 1.25 mg/mL (1.20 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: 1.25 mg/mL (1.20 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (271 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]. Donovan KA, et al. Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development. Cell. 2020 Dec 10;183(6):1714-1731.e10. [Content Brief]
[2]. Zhou M, et al. HUWE1 amplifies ubiquitin modifications to broadly stimulate clearance of proteins and aggregates[J]. BioRxiv, 2023: 2023.05. 30.542866. [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 (stored under nitrogen). 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 | 0.9606 mL | 4.8028 mL | 9.6057 mL | 24.0142 mL |
| 5 mM | 0.1921 mL | 0.9606 mL | 1.9211 mL | 4.8028 mL | |
| 10 mM | 0.0961 mL | 0.4803 mL | 0.9606 mL | 2.4014 mL | |
| 15 mM | 0.0640 mL | 0.3202 mL | 0.6404 mL | 1.6009 mL | |
| 20 mM | 0.0480 mL | 0.2401 mL | 0.4803 mL | 1.2007 mL | |
| 25 mM | 0.0384 mL | 0.1921 mL | 0.3842 mL | 0.9606 mL | |
| 30 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8005 mL | |
| 40 mM | 0.0240 mL | 0.1201 mL | 0.2401 mL | 0.6004 mL |
DB-0646 関連分類
HY-137343 関連分類
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