| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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Purity: ≥98%
| Targets |
PROTAC BET Degrader-3 targets BET proteins, including BRD2, BRD3, and BRD4. BET proteins are epigenetic readers that recognize acetylated lysine residues on histone tails and regulate the transcription of genes involved in cell cycle progression, inflammation, and oncogenesis. By inducing the degradation of BET proteins, the compound effectively removes these transcriptional regulators from cells, leading to downregulation of oncogenic gene expression programs.
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| ln Vitro |
In vitro, PROTAC BET Degrader-3 potently induces the degradation of BET proteins in cancer cell lines. The compound recruits an E3 ubiquitin ligase to BET proteins, leading to their ubiquitination and proteasomal degradation. This results in the suppression of BET-dependent gene transcription, including downregulation of oncogenes such as c-Myc. The compound demonstrates potent antiproliferative activity against various cancer cell lines.
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| ln Vivo |
In vivo, PROTAC BET Degrader-3 has the potential to exhibit antitumor activity by degrading BET proteins in tumor tissues. As a PROTAC-based degrader, it offers advantages over traditional inhibitors, including sustained target suppression and the ability to target non-enzymatic functions of BET proteins. Preclinical studies are expected to demonstrate its efficacy in tumor xenograft models.
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| Enzyme Assay |
In vitro degradation assays are performed using cancer cell lines treated with PROTAC BET Degrader-3 at various concentrations (typically 0.1-1000 nM) for 4-24 hours. BET protein levels (BRD2, BRD3, BRD4) are measured by Western blot using specific antibodies. The DC₅₀ (concentration for 50% degradation) is calculated from dose-response curves. Proteasome inhibition studies using MG132 confirm that degradation is proteasome-dependent.
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| Cell Assay |
Cellular assays are performed using cancer cell lines such as MV4-11 (acute myeloid leukemia) or other BET-dependent cancer cells. Cells are treated with PROTAC BET Degrader-3 at various concentrations for 48-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Downstream effects on gene expression are evaluated by qPCR for BET target genes such as c-Myc and PIM1.
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| Animal Protocol |
In vivo studies are conducted in tumor-bearing mouse models. PROTAC BET Degrader-3 is administered intravenously or intraperitoneally at various doses. Tumor volume is measured periodically, and tumors are harvested for Western blot analysis of BET protein levels to confirm target degradation. Pharmacokinetic parameters and biomarker analysis are performed to assess the compound's in vivo activity.
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| ADME/Pharmacokinetics |
PROTAC BET Degrader-3 (molecular weight 1045.22, formula C₅₃H₆₄N₁₂O₉S) is a PROTAC molecule. It is soluble in DMSO (100 mg/mL, 95.67 mM) with sonication and is insoluble in water. The compound should be stored at -20°C for long-term stability (months to years) or at 2-8°C for short-term use (days to weeks).
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of PROTAC BET Degrader-3 have been limited, as the compound is primarily used as a research tool. As a BET degrader, its toxicity profile is expected to be related to the biological effects of BET protein degradation, including potential effects on normal cell proliferation and differentiation. No significant toxicity has been reported in the available literature.
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| References |
N/A
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| Additional Infomation |
PROTAC BET Degrader-3 is a potent BET protein degrader based on PROTAC technology. Its mechanism involves recruiting an E3 ubiquitin ligase to BET proteins, leading to their ubiquitination and proteasomal degradation. The compound is primarily used as a research tool to study the biological functions of BET proteins and to explore the therapeutic potential of BET degradation in cancer and other diseases. PROTAC BET Degrader-3 has not received regulatory approval for clinical use.
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| Molecular Formula |
C₂₇H₂₉CL₂N₇O₂S
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|---|---|
| Molecular Weight |
586.54
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| Appearance |
Light yellow to yellow solid powder
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| SMILES |
O=C(NCC1=CC=C(S(C2=CC(F)=CC(F)=C2)(=O)=O)C=C1)C3=CN4C(C=C3)=NC=C4.Cl
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| Synonyms |
PROTAC BET degrader-3; PROTAC BET degrader 3
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7049 mL | 8.5246 mL | 17.0491 mL | |
| 5 mM | 0.3410 mL | 1.7049 mL | 3.4098 mL | |
| 10 mM | 0.1705 mL | 0.8525 mL | 1.7049 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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