| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
PROTAC BRD4 Degrader-11 targets BRD4. It is a chimeric molecule that contains a ligand for BRD4 and a ligand for the von Hippel-Lindau (VHL) E3 ubiquitin ligase. It is specifically designed to be conjugated to antibodies to form ADCs. When internalized into target cells, it induces the degradation of BRD4. It targets BRD4 protein in PC3 prostate cancer cells.
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| ln Vitro |
In vitro, PROTAC BRD4 Degrader-11 can be conjugated to STEAP1 and CLL1 antibodies. When these antibody-degrader conjugates are used to treat PC3 prostate cancer cells, they degrade BRD4 with high efficiency, demonstrating DC50 values of 0.23 nM and 0.38 nM, respectively. PROTAC BRD4 Degrader-11 effectively targets and degrades the BRD4 protein in PC3 cells.
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| ln Vivo |
PROTAC BRD4 Degrader-11 itself is a highly potent degrader, but as an ADC payload, its in vivo activity is conferred by the antibody conjugate. In mouse xenograft models, ADCs bearing PROTAC BRD4 Degrader-11 have demonstrated improved in vitro antiproliferation activity and in vivo antitumor efficacy.
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| Enzyme Assay |
PROTAC BRD4 Degrader-11 is a complete PROTAC, not just a ligand. Its activity is typically assessed in cell-based assays rather than cell-free systems. It is designed to recruit the VHL E3 ligase to induce BRD4 degradation via the ubiquitin-proteasome pathway, which requires a functional cellular degradation machinery.
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| Cell Assay |
PC3 prostate cancer cells are seeded in 6-well plates and treated with antibody-conjugated PROTAC BRD4 Degrader-11 for 4-24 hours. After treatment, cells are lysed, and protein lysates are analyzed by Western blot with an anti-BRD4 antibody. Densitometry is used to quantify the reduction in BRD4 protein levels, and the DC50 is calculated from the concentration-response curve.
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| Animal Protocol |
A standard in vivo animal protocol for PROTAC BRD4 Degrader-11 is not typical for the degrader alone. As an ADC payload, it would be conjugated to an antibody. In a mouse xenograft model, mice are injected with tumor cells (e.g., PC3). Once tumors are established, they are treated with the ADC. Tumor growth inhibition is measured, and BRD4 degradation in tumor tissues is confirmed by IHC.
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| ADME/Pharmacokinetics |
PROTAC BRD4 Degrader-11 has a molecular weight of 1292.5 and the formula C61H75F2N9O12S4. It is a solid compound that should be stored at -20degC, sealed and away from moisture and light. In solvent, it is stable for 6 months at -80degC. Specific PK data are not available.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for PROTAC BRD4 Degrader-11 have not been reported. As a research chemical, standard laboratory safety precautions should be followed. Its safety profile would be more relevant when conjugated to an antibody as an ADC. The small molecule itself is handled as a potent biological research tool.
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| References | |
| Additional Infomation |
PROTAC BRD4 Degrader-11 is a research-grade chemical and is not approved for clinical use. It is a potent PROTAC that can be conjugated to STEAP1 and CLL1 antibodies for targeted delivery to degrade BRD4 in prostate cancer cells. It is a valuable tool for antibody-drug conjugate (ADC) research and development. It is a pure chemical tool designed for specific applications in targeted protein degradation.
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| Molecular Formula |
C61H75F2N9O12S4
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|---|---|
| Molecular Weight |
1292.56
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| Appearance |
Off-white to light yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~100 mg/mL (~77.37 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7737 mL | 3.8683 mL | 7.7366 mL | |
| 5 mM | 0.1547 mL | 0.7737 mL | 1.5473 mL | |
| 10 mM | 0.0774 mL | 0.3868 mL | 0.7737 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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