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| 10mg |
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| Targets |
BRD4 Inhibitor-24 targets the bromodomain-containing protein 4 (BRD4), an epigenetic reader domain that recognizes acetylated lysine residues on histone tails. BRD4 plays a critical role in regulating gene transcription, including oncogenes such as MYC. By inhibiting BRD4, this compound disrupts the interaction between BRD4 and acetylated histones, thereby modulating the expression of genes involved in cell proliferation and survival. The compound's mechanism of action is consistent with that of other BRD4 inhibitors being investigated as potential anticancer agents.
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| ln Vitro |
In vitro, BRD4 Inhibitor-24 demonstrates antiproliferative activity against cancer cell lines. It exhibits an IC₅₀ of 33.7 μM against MCF7 cells and 45.9 μM against K652 cells. These values indicate its potency in inhibiting cell viability in these models. The compound's activity is derived from patent CN107721975A, which describes its synthesis and antitumor properties. Further details on its mechanism of action, such as effects on BRD4-dependent transcription or downstream signaling pathways, are not extensively detailed in the available sources.
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| ln Vivo |
Specific in vivo activity data for BRD4 Inhibitor-24 are not provided in the available sources. As a research compound primarily described in a patent, its in vivo efficacy, pharmacokinetics, and pharmacodynamics in animal models have not been detailed in the accessible literature. The compound is intended for research use to explore the role of BRD4 in cancer biology, suggesting that further preclinical studies would be necessary to evaluate its in vivo potential. Its antitumor activity has been demonstrated only in cell-based assays to date.
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| Enzyme Assay |
A cell-free assay for BRD4 Inhibitor-24 would typically involve evaluating its binding affinity to the BRD4 bromodomain using techniques such as fluorescence polarization, AlphaScreen, or surface plasmon resonance (SPR). These assays measure the compound's ability to displace a labeled acetylated histone peptide from the BRD4 protein. However, specific IC₅₀ values from such cell-free assays are not provided in the available sources. The compound's activity has been characterized primarily in cell-based viability assays.
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| Cell Assay |
A typical in vitro cell viability assay for BRD4 Inhibitor-24 involves culturing cancer cell lines such as MCF7 (breast cancer) or K652 (leukemia) in appropriate media. Cells are seeded in 96-well plates and treated with varying concentrations of the compound for a specified duration (e.g., 48-72 hours). Cell viability is then assessed using a standard assay such as MTT, CCK-8, or resazurin reduction. The IC₅₀ values are calculated from dose-response curves. For BRD4 Inhibitor-24, the reported IC₅₀ values are 33.7 μM for MCF7 and 45.9 μM for K652 cells.
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| Animal Protocol |
Specific in vivo animal实验 protocols for BRD4 Inhibitor-24 are not described in the available sources. As a compound primarily characterized in vitro, its in vivo evaluation would typically involve xenograft models in immunocompromised mice. In such a study, tumor-bearing mice would be administered the compound via oral gavage or intraperitoneal injection at various doses. Tumor volume and body weight would be monitored regularly to assess efficacy and tolerability. However, no such data or protocols are available from the provided references.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of BRD4 Inhibitor-24 are not reported in the available sources. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) profiles have not been characterized in the accessible literature. General storage recommendations for the compound include keeping it at 4°C, protected from light. Stock solutions should be stored at -80°C for up to 6 months or at -20°C for up to 1 month to prevent degradation. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Toxicity data for BRD4 Inhibitor-24 are not provided in the available sources. As with many research compounds, detailed toxicological profiles are typically established during later stages of drug development. The compound is intended for research use only and is not for human consumption. Safety precautions should be observed when handling, including the use of appropriate personal protective equipment. Its cytotoxicity against cancer cell lines suggests it has antiproliferative effects, but this does not necessarily translate to in vivo toxicity.
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| References | |
| Additional Infomation |
BRD4 Inhibitor-24 (CAS: 309951-18-6) is a research compound derived from patent CN107721975A, which describes its synthesis and antitumor activity. Its molecular formula is C₁₃H₁₄N₂O₄ with a molecular weight of 262.26. The compound is also known as compound 3U. It is not an approved drug and has not undergone clinical trials. Its primary value lies in its use as a tool compound for studying BRD4 biology and evaluating the potential of BRD4 inhibition as a therapeutic strategy in cancer. The compound is available from various research chemical suppliers for non-clinical research purposes only.
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| Molecular Formula |
C13H14N2O4
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|---|---|
| Molecular Weight |
262.261
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| Exact Mass |
262.095
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| CAS # |
309951-18-6
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| PubChem CID |
694790
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
313
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C(C(NC2=NOC(C)=C2)=O)C=C1OC
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| InChi Key |
LZELTTNSPNYMCU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H14N2O4/c1-8-6-12(15-19-8)14-13(16)9-4-5-10(17-2)11(7-9)18-3/h4-7H,1-3H3,(H,14,15,16)
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| Chemical Name |
3,4-dimethoxy-N-(5-methyl-1,2-oxazol-3-yl)benzamide
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~381.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.53 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 | 3.8130 mL | 19.0650 mL | 38.1301 mL | |
| 5 mM | 0.7626 mL | 3.8130 mL | 7.6260 mL | |
| 10 mM | 0.3813 mL | 1.9065 mL | 3.8130 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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