| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
CPI-268456 targets bromodomain-containing protein 4 (BRD4). It acts as an inhibitor, binding to the bromodomain of BRD4 and preventing its interaction with acetylated histones. This inhibits BRD4's function as a transcriptional coactivator, leading to the downregulation of oncogenes and other target genes. BRD4 is a well-validated target in cancer, particularly in hematological malignancies and certain solid tumors.
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| ln Vitro |
In vitro, CPI-268456 binds to BRD4 with an IC50 of less than 0.5 µM. It also inhibits LPS-induced IL-6 secretion in THP-1 cells with an IC50 of less than 0.5 µM. This demonstrates its ability to inhibit BRD4 function and modulate inflammatory responses. Its activity as a BRD4 inhibitor makes it a valuable tool for studying the role of BRD4 in gene regulation and disease.
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| ln Vivo |
In vivo activity data for CPI-268456 is limited. As a BRD4 inhibitor, it is expected to have antitumor and anti-inflammatory effects in animal models. However, specific in vivo study details are not well-documented. It is primarily used as a research tool to study the function of BRD4 in various biological processes.
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| Enzyme Assay |
CPI-268456 is evaluated in cell-free assays to measure its binding affinity for BRD4. The compound is incubated with BRD4 protein, and the binding is measured using techniques such as fluorescence polarization or surface plasmon resonance. IC50 values are determined to quantify the potency of BRD4 binding.
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| Cell Assay |
CPI-268456 is assessed in cell-based assays using THP-1 cells. Cells are treated with LPS to induce IL-6 secretion, and then incubated with CPI-268456. The inhibition of IL-6 secretion is measured, and IC50 values are determined. This assay confirms its ability to inhibit BRD4 function in a cellular context. Its effects on cell proliferation and gene expression can also be evaluated in cancer cell lines.
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| Animal Protocol |
CPI-268456 is administered in animal models to evaluate its effects on BRD4-mediated functions. However, specific animal study protocols are not extensively documented. It is typically formulated for in vivo administration using DMSO or other suitable vehicles. Its efficacy in models of cancer or inflammation is of research interest.
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| ADME/Pharmacokinetics |
CPI-268456 has a molecular formula of C20H15Cl2N3O2 and a molecular weight of 400.26. Its CAS number is 1380087-86-4. The compound is soluble in DMSO. It should be stored under recommended conditions. It is also known as BRD4-IN-3.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CPI-268456. The compound is for research use only and is not intended for human therapeutic use. It is a potent BRD4 inhibitor used as a research tool to study epigenetics and gene regulation.
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| Additional Infomation |
CPI-268456 is a potent inhibitor of BRD4. It is also known as BRD4-IN-3. It is used in research to study the role of BRD4 in gene regulation, cancer, and inflammation. The compound is not approved for clinical use.
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| Molecular Formula |
C20H15N3O2CL2
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|---|---|
| Molecular Weight |
400.258
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| Exact Mass |
399.054
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| CAS # |
1380087-86-4
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| Related CAS # |
1380087-86-4;
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| PubChem CID |
57389997
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
649.8±55.0 °C at 760 mmHg
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| Flash Point |
346.8±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.702
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| LogP |
3.42
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
594
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| Defined Atom Stereocenter Count |
1
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| SMILES |
NC(C[C@H]1N=C(C2=CC=C(Cl)C=C2)C2=CC(=CC=C2C2C(=NOC1=2)C)Cl)=O
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| InChi Key |
RKYPLOAYXFDLOF-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C20H15Cl2N3O2/c1-10-18-14-7-6-13(22)8-15(14)19(11-2-4-12(21)5-3-11)24-16(9-17(23)26)20(18)27-25-10/h2-8,16H,9H2,1H3,(H2,23,26)/t16-/m0/s1
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| Chemical Name |
2-[(4S)-8-chloro-6-(4-chlorophenyl)-1-methyl-4H-[1,2]oxazolo[5,4-d][2]benzazepin-4-yl]acetamide
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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 | 2.4984 mL | 12.4919 mL | 24.9838 mL | |
| 5 mM | 0.4997 mL | 2.4984 mL | 4.9968 mL | |
| 10 mM | 0.2498 mL | 1.2492 mL | 2.4984 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.
Products are for research use only; We do not sell to patients
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