PROTAC BRD4 Degrader linker conjugate-3
Based on 1 Customer Validation
PROTAC BRD4 Degrader linker conjugate-3 is a VHL-recruiting PROTAC that targets and degrades BRD4. It can be used in studies related to prostate cancer.
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- Pureté: 98.54%
- CAS No.: 2417370-90-0
- Formule: C62H77F2N9O12S4
- Masse moléculaire:1306.58
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Stockage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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BRD4 |
VHL |
PROTAC BRD4 Degrader linker conjugate-3 (compound 9c) binds to BRD4 BD2 bromodomain with an IC50 of 69 nM[1].
PROTAC BRD4 Degrader linker conjugate-3 binds to VHL with an IC50 of 135 nM[1].
PROTAC BRD4 Degrader linker conjugate-3 suppresses MYC gene transcript levels in MV4-11 AML cells by 97% at maximum effect, with an IC50 of 86 nM[1].
PROTAC BRD4 Degrader linker conjugate-3 (4 hours) reduces BRD4 protein levels in PC3-S1 prostate cancer cells by 98% at maximum effect, with a DC50 of 85 nM following 4 hours of incubation[1].
PROTAC BRD4 Degrader linker conjugate-3 (6 days) inhibits PC3-S1 prostate cancer cell proliferation with an IC50 of 1300 nM following 6 days of incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2417370-90-0
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Appearance Solid
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Masse moléculaire 1306.58
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Formule C62H77F2N9O12S4
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Color White to light yellow
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SMILES
CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@H](CN3C([C@@H](NC(CCCCCCCCCCNC(C4=CC(N(C5=NC=C(F)C=C5F)CC6=CNC7=C6C8=CN(C)C7=O)=C8C=C4CS(=O)(C)=O)=O)=O)C(C)(C)C)=O)OC(OC(C)C(C)SS(C)(=O)=O)=O)=O)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : 100 mg/mL (76.54 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 3.25 mg/mL (2.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3.25 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 (32.5 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.
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 (sealed storage, away from moisture and 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.
Pureté et documentation
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Fiche technique (272 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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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture and 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 | 0.7654 mL | 3.8268 mL | 7.6536 mL | 19.1339 mL |
| 5 mM | 0.1531 mL | 0.7654 mL | 1.5307 mL | 3.8268 mL | |
| 10 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9134 mL | |
| 15 mM | 0.0510 mL | 0.2551 mL | 0.5102 mL | 1.2756 mL | |
| 20 mM | 0.0383 mL | 0.1913 mL | 0.3827 mL | 0.9567 mL | |
| 25 mM | 0.0306 mL | 0.1531 mL | 0.3061 mL | 0.7654 mL | |
| 30 mM | 0.0255 mL | 0.1276 mL | 0.2551 mL | 0.6378 mL | |
| 40 mM | 0.0191 mL | 0.0957 mL | 0.1913 mL | 0.4783 mL | |
| 50 mM | 0.0153 mL | 0.0765 mL | 0.1531 mL | 0.3827 mL | |
| 60 mM | 0.0128 mL | 0.0638 mL | 0.1276 mL | 0.3189 mL |
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