PROTAC BRD4 Degrader linker conjugate-2
Based on 1 Customer Validation
PROTAC BRD4 Degrader linker conjugate-2 is a PROTAC-based BRD4 degrader.
For research use only. We do not sell to patients.
- Purity: 99.75%
- CAS No.: 2417370-49-9
- Formula: C59H71F2N9O15S4
- Molecular Weight:1312.50
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from 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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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BRD4 |
PROTAC BRD4 Degrader linker conjugate-2 (compound 8b) (4 h) suppresses MYC gene transcript levels in MV4-11 AML cells by 98% at maximum inhibition, with an IC50 of 11 nM after 4 hours of incubation[1].
PROTAC BRD4 Degrader linker conjugate-2 (4 h) degrades BRD4 protein in PC3-S1 prostate cancer cells by 98% relative to DMSO controls, with a DC50 of 7.5 nM after 4 hours of incubation[1].
PROTAC BRD4 Degrader linker conjugate-2 (6 day) inhibits PC3-S1 prostate cancer cell proliferation with an IC50 of 28 nM after 6 days of incubation[1].
PROTAC BRD4 Degrader linker conjugate-2 (6 day) inhibits HL-60 acute myeloid leukemia cell proliferation with an IC50 of 1.9 nM after 6 days of incubation[1].
PROTAC BRD4 Degrader linker conjugate-2 (6 day) inhibits proliferation in PC3-S1 and LNCaP prostate cancer cell lines with an average IC50 of 17.9 nM after 6 days of incubation[1].
PROTAC BRD4 Degrader linker conjugate-2 (6 day) inhibits proliferation in HL-60 and EOL-1 AML cell lines with an average IC50 of 1.91 nM after 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. 2417370-49-9
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Appearance Solid
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Molecular Weight 1312.50
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Formula C59H71F2N9O15S4
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Color Off-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(COCCOCCOCCNC(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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 200 mg/mL (152.38 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.
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: ≥ 5 mg/mL (3.81 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.
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.
Purity & Documentation
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Data Sheet (273 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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Handling Instructions (2659 KB)
References
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 | 0.7619 mL | 3.8095 mL | 7.6190 mL | 19.0476 mL |
| 5 mM | 0.1524 mL | 0.7619 mL | 1.5238 mL | 3.8095 mL | |
| 10 mM | 0.0762 mL | 0.3810 mL | 0.7619 mL | 1.9048 mL | |
| 15 mM | 0.0508 mL | 0.2540 mL | 0.5079 mL | 1.2698 mL | |
| 20 mM | 0.0381 mL | 0.1905 mL | 0.3810 mL | 0.9524 mL | |
| 25 mM | 0.0305 mL | 0.1524 mL | 0.3048 mL | 0.7619 mL | |
| 30 mM | 0.0254 mL | 0.1270 mL | 0.2540 mL | 0.6349 mL | |
| 40 mM | 0.0190 mL | 0.0952 mL | 0.1905 mL | 0.4762 mL | |
| 50 mM | 0.0152 mL | 0.0762 mL | 0.1524 mL | 0.3810 mL | |
| 60 mM | 0.0127 mL | 0.0635 mL | 0.1270 mL | 0.3175 mL | |
| 80 mM | 0.0095 mL | 0.0476 mL | 0.0952 mL | 0.2381 mL | |
| 100 mM | 0.0076 mL | 0.0381 mL | 0.0762 mL | 0.1905 mL |
PROTAC BRD4 Degrader linker conjugate-2 Related Classifications
HY-138633 Related Classifications
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- PROTAC BRD4 Degrader linker conjugate-2
- 2417370-49-9
- PROTACs
- Epigenetic Reader Domain
- HL-60 acute myeloid leukemia cells
- LNCaP prostate cancer cell lines
- BRD4
- EOL-1 AML cell lines
- proteolysis-targeting chimera
- PC3-S1 prostate cancer cells
- antibody-drug conjugates
- MV4-11 AML cells
- MYC gene
- Inhibitor
- inhibitor
- inhibit