| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
EF24 targets multiple pathways. It inhibits IKK (IκB kinase), leading to inhibition of NF-κB activation. It also inhibits the MAPK/ERK signaling pathway by reducing the expression of phosphorylated MEK1 and ERK. By blocking these pathways, EF24 induces cell cycle arrest and apoptosis in cancer cells. It increases the levels of activated caspase-3 and caspase-9.
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| ln Vitro |
In vitro, EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. It induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. It inhibits MAPK/ERK signaling by reducing phosphorylated MEK1 and ERK. It increases activated caspase-3 and caspase-9 levels.
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| ln Vivo |
In vivo, EF24 is orally bioavailable. It inhibits tumor growth and metastasis by blocking NF-κB-dependent signaling pathways. It is more efficacious in anti-cancer screens and less toxic than cisplatin. The compound's oral bioavailability supports its use in in vivo efficacy studies. Further preclinical studies would evaluate its antitumor activity in xenograft models.
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| Enzyme Assay |
In vitro enzyme assays for EF24 measure IKK inhibition using recombinant IKK enzyme. Kinase activity is assessed by measuring phosphorylation of IκBα or a peptide substrate. NF-κB inhibition is assessed using reporter cell lines with NF-κB-driven luciferase expression. Various concentrations of EF24 are added. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for EF24 use cancer cell lines such as MDA-MB-231, DU-145, and melanoma cells. Cells are treated with various concentrations of EF24. Cell viability is measured using MTT or ATP-lite assays. Cell cycle analysis is performed by flow cytometry. Apoptosis is assessed by caspase-3/7 activity or Annexin V staining. MAPK/ERK signaling is assessed by Western blotting.
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| Animal Protocol |
In vivo animal studies for EF24 utilize tumor xenograft models in mice. The compound is administered orally at various doses. Tumor volume is measured over time. NF-κB activation, MAPK/ERK signaling, and apoptosis markers are assessed in tumor tissue. Efficacy is compared to vehicle and reference anticancer agents (e.g., cisplatin).
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| ADME/Pharmacokinetics |
EF24 has molecular weight of approximately 327.4 g/mol and molecular formula C17H12F2N2O·HCl. It is a hydrochloride salt. It is typically stored at -20°C. It is soluble in DMSO. It is orally bioavailable. Pharmacokinetic properties support once-daily oral dosing. The compound is a synthetic curcumin analog.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of EF24 has been evaluated in standard toxicology studies. It is less toxic than cisplatin. As an NF-κB and IKK inhibitor, potential adverse effects may include gastrointestinal effects and immunosuppression. No significant toxicity has been reported at therapeutic doses. The compound is for research use only.
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| References | |
| Additional Infomation |
EF24 is a synthetic curcumin analog with enhanced antitumor efficacy. It inhibits IKK and NF-κB. It induces apoptosis in cancer cells. It is more potent than curcumin and less toxic than cisplatin. It is available for research purposes only.
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| Molecular Formula |
C19H16CLF2NO
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|---|---|
| Molecular Weight |
347.79
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| Exact Mass |
347.089
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| CAS # |
342808-40-6
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| Related CAS # |
342808-40-6 (hydrochloride);917813-75-3;
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| PubChem CID |
9885748
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| Appearance |
White to yellow solid powder
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| LogP |
4.734
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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 |
2
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| Heavy Atom Count |
23
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| Complexity |
458
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C\1NC/C(=C\C2=CC=CC=C2F)/C(=O)/C1=C/C3=CC=CC=C3F
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| InChi Key |
NIVYQYSNRUIFIF-KAVGSWPWSA-N
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| InChi Code |
InChI=1S/C19H15F2NO/c20-17-7-3-1-5-13(17)9-15-11-22-12-16(19(15)23)10-14-6-2-4-8-18(14)21/h1-10,22H,11-12H2/b15-9+,16-10+
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| Chemical Name |
(3E,5E)-3,5-bis[(2-fluorophenyl)methylidene]piperidin-4-one
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| Synonyms |
EF-24; EF 24; EF24
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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) |
DMSO : ~50 mg/mL (~160.60 mM)
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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 | 2.8753 mL | 14.3765 mL | 28.7530 mL | |
| 5 mM | 0.5751 mL | 2.8753 mL | 5.7506 mL | |
| 10 mM | 0.2875 mL | 1.4376 mL | 2.8753 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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