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| 1mg |
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| 5mg |
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| Targets |
CLEFMA targets NF-κB signaling pathways. By inhibiting NF-κB-regulated inflammatory and metastatic processes, the compound suppresses tumor growth. The compound's mechanism involves both anti-inflammatory and anti-metastatic effects. CLEFMA induces apoptosis in cancer cells. As a curcumin analog, it shares structural features with curcumin but has enhanced activity.
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| ln Vitro |
CLEFMA possesses anti-proliferative action (1-100 μM; 24-72 h)[1]. H441 and A549 cells' viability is inhibited by CLEFMA, with IC50s of 6.4 and 8.9 μM, respectively[2]. H441 and A549 cells undergo apoptosis when exposed to CLEFMA (5–10 μM; 24 h)[2]. In H441 cells, CLEFMA (1 and 10 μM; 24 h) causes autophagic death[1]. CLEFMA (1–20 μM) dose-dependently decreases NF-κB's DNA-binding activity in H441 cells[2].
In vitro studies demonstrate that CLEFMA (1-100 μM; 24-72 h) has anti-proliferative activity. The compound inhibits the viability of H441 and A549 lung adenocarcinoma cells with IC50 values of 6.4 and 8.9 μM, respectively. When exposed to CLEFMA (5-10 μM; 24 h), H441 and A549 cells undergo apoptosis. CLEFMA dose-dependently decreases the cell viabilities of human osteosarcoma U2OS and HOS cells and significantly induces apoptosis. The compound has been investigated in lung adenocarcinoma H441 and A549, and normal lung fibroblast CCL151 cell lines. |
| ln Vivo |
In a xenograft mouse model, CLEFMA (0.2-0.4 mg/kg; ip daily for 4 weeks) suppresses the uptake of FDG in tumor tissue and inhibits tumor growth[2]. Pro-apoptotic protein BID is cleaved and pro-apoptotic BAX is expressed in tumor tissue when CLEFMA (0.2–0.4 mg/kg; intraperitoneal; daily for 4 weeks) is administered. It also downregulates the expression of anti-apoptotic markers cIAP1, Bcl-xL, Bcl-2, and survivin[2].
In vivo, CLEFMA has demonstrated tumor suppression in a xenograft model of H441 cells implanted in mice. The compound inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects. CLEFMA induces apoptosis and inflammatory markers during tumor suppression. The compound's in vivo efficacy has been demonstrated in mouse xenograft models. |
| Enzyme Assay |
The NF-κB inhibitory activity of CLEFMA can be assessed using reporter assays or by measuring NF-κB target gene expression. In a typical assay, cells are treated with varying concentrations of CLEFMA, and NF-κB activation is measured by luciferase reporter assay or by Western blotting for NF-κB target proteins. The anti-proliferative activity is assessed using MTT or CellTiter-Glo assays. Apoptosis is measured by annexin V/propidium iodide staining or caspase activation assays.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: PANC-1, MiaPaCa -2, PC-3 and H441 cells Tested Concentrations: 1, 10, 25, 100 μM Incubation Duration: 24, 48, 72 h Experimental Results: Inhibits cell proliferation in a dose-dependent manner. The cellular activity of CLEFMA is assessed using various cancer cell lines including lung adenocarcinoma H441 and A549, osteosarcoma U2OS and HOS, and normal lung fibroblast CCL151 cells. Cells are treated with CLEFMA (1-100 μM; 24-72 h). Cell viability is measured using MTT assays, and IC50 values are calculated. Apoptosis is assessed by annexin V/propidium iodide staining. NF-κB target gene expression is measured by qPCR or Western blotting. |
| Animal Protocol |
Animal/Disease Models: Male athymic nu/nu (nude) mice (4 weeks old) are injected H441 cells[2]
Doses: 0.2, 0.4 mg/kg Route of Administration: Ip daily for 4 weeks Experimental Results: Inhibited tumor growth up to 96% tumor at dose of 0.4 mg/kg. CLEFMA has been evaluated in a xenograft model of H441 lung adenocarcinoma cells implanted in mice. In this model, tumor-bearing mice are treated with CLEFMA, and tumor volumes are measured. The compound inhibits tumor growth. Changes in apoptosis and inflammatory markers are investigated during CLEFMA-induced tumor suppression. The compound's anti-metastatic effects can be assessed in appropriate metastasis models. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published for CLEFMA. The compound has a molecular weight of approximately 454.3 g/mol and a molecular formula of C23H17Cl2NO4. As a curcumin analog, it is likely to have moderate oral bioavailability and metabolic stability. Further studies would be needed to characterize its absorption, distribution, metabolism, and excretion properties, including plasma protein binding, clearance, and half-life.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for CLEFMA. In vitro studies using normal lung fibroblast CCL151 cells suggest that the compound may have some selectivity for cancer cells. As a curcumin analog, it may have a favorable safety profile, but comprehensive toxicology studies would be required to evaluate its safety for potential therapeutic development. The compound is intended for research use only.
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| References |
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| Additional Infomation |
CLEFMA (CAS# 1246964-32-8) is a curcumin analog with anti-tumor activity. It inhibits the viability of H441 and A549 lung adenocarcinoma cells with IC50 values of 6.4 and 8.9 μM, respectively. The compound induces apoptosis and inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects. CLEFMA also decreases the viability of osteosarcoma U2OS and HOS cells. It has been evaluated in a xenograft model of H441 cells. The molecular formula is C23H17Cl2NO4.
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| Molecular Formula |
C23H17CL2NO4
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| Exact Mass |
441.053
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| CAS # |
1246964-32-8
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| PubChem CID |
46927962
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.1
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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 |
4
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| Heavy Atom Count |
30
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| Complexity |
729
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C\1N(C/C(=C\C2=CC=CC=C2Cl)/C(=O)/C1=C/C3=CC=CC=C3Cl)C(=O)/C=C\C(=O)O
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| InChi Key |
ABOUDPJRQGWQNW-GGDLZHBGSA-N
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| InChi Code |
InChI=1S/C23H17Cl2NO4/c24-19-7-3-1-5-15(19)11-17-13-26(21(27)9-10-22(28)29)14-18(23(17)30)12-16-6-2-4-8-20(16)25/h1-12H,13-14H2,(H,28,29)/b10-9-,17-11+,18-12+
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| Chemical Name |
(Z)-4-[(3E,5E)-3,5-bis[(2-chlorophenyl)methylidene]-4-oxopiperidin-1-yl]-4-oxobut-2-enoic acid
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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.) |
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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