| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Ceefourin-1 targets multidrug resistance protein 4 (MRP4/ABCC4), an ATP-binding cassette (ABC) transporter that mediates the efflux of various endogenous and exogenous substrates, including cyclic nucleotides, prostaglandins, and chemotherapeutic agents. By inhibiting MRP4, Ceefourin-1 potentiates the accumulation of MRP4 substrates and reverses MRP4-mediated drug resistance.
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| ln Vitro |
Ceefourin 1 affects MRP4 of additional ABC transporters, such as MRP1 (ABCC1), P-glycoprotein (P-gp), and ABCG2 (breast cancer protein; BCRP). Ceefourin 1 has good stability and negligible off-target effects. Ceffourin 1 (100 nM-100 μM) exhibits efficacy against seven neuroblastoma cells (BE(2)-C, IMR-32, LAN-1) as well as two normal cells (HSF, MRC5). IMR-32, SK). Four more human liver lines (HEPG2, LNCap, SJ-G2, MCF7) and -N-SH, NBL-WN, and SHEP) exhibit low cytotoxicity (IC50>50) [1]. In HEK293 cells, Ceefourin 1 has an IC50 of 2.5 μM. With an IC50 of 1.5 μM, ceftetraline 1 inhibits D-luciferin breakthrough [1].
In vitro, Ceefourin-1 potentiates global cytosolic cAMP accumulation in BE(2)-C neuroblastoma cells following forskolin stimulation. It reverses 6-mercaptopurine (6-MP) resistance conferred by MRP4 in HEK293-MRP4 cells, and is more potent than MK-571. Ceefourin-1 exhibits no activity against cell lines overexpressing P-gp (HEK293-Pgp), ABCG2 (HEK293-ABCG2), or MRP1 (MCF7-VP16). |
| ln Vivo |
In vivo, Ceefourin-1 has been studied for its ability to modulate MRP4-mediated transport and reverse drug resistance. As a selective MRP4 inhibitor, it may enhance the efficacy of MRP4-substrate chemotherapeutic agents. Specific in vivo data including efficacy in tumor models and PK profiles are available from published studies.
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| Enzyme Assay |
In vitro transporter assays for MRP4 inhibition typically use membrane vesicles prepared from cells overexpressing MRP4 or whole cells expressing MRP4. The transport of a fluorescent or radiolabeled MRP4 substrate (e.g., [³H]cAMP, [³H]E217βG, or a fluorescent probe) is measured in the presence of varying concentrations of Ceefourin-1. IC50 values for inhibition of substrate transport are calculated from dose-response curves.
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| Cell Assay |
In vitro cellular assays for MRP4 inhibitors typically use HEK293 cells stably expressing MRP4 or other cell lines with endogenous MRP4 expression. Cells are treated with Ceefourin-1 at various concentrations, and the intracellular accumulation of a fluorescent MRP4 substrate is measured by flow cytometry or fluorescence microscopy. The degree of reversal of MRP4-mediated drug resistance is assessed using cytotoxicity assays.
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| Animal Protocol |
In vivo animal studies for MRP4 inhibitors typically use xenograft tumor models in immunocompromised mice. Animals are implanted with MRP4-overexpressing tumor cells and treated with Ceefourin-1 alone or in combination with an MRP4-substrate chemotherapeutic agent. Tumor growth is monitored, and the compound's ability to reverse drug resistance and enhance antitumor efficacy is assessed.
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| ADME/Pharmacokinetics |
Ceefourin-1 has a molecular weight of 294.42 and is soluble in DMSO (10 mM). It demonstrates good stability and negligible off-target effects. The compound is relatively non-toxic and well tolerated across a broad range of cell lines, with IC50 values typically >50 μM. Detailed PK parameters are available from published studies.
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| Toxicity/Toxicokinetics |
Ceefourin-1 is relatively non-toxic and well tolerated across a broad range of cell lines, with IC50 values typically >50 μM. It shows no significant cytotoxicity at concentrations required for MRP4 inhibition. Standard toxicity assessments would include acute and repeated-dose toxicity in rodents, as well as genotoxicity evaluations.
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| References |
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| Additional Infomation |
Ceefourin-1 is a potent and highly selective inhibitor of MRP4/ABCC4. It inhibits the efflux of MRP4 substrates and reverses MRP4-mediated drug resistance. The compound is selective for MRP4 over other ABC transporters and is relatively non-toxic. It is a valuable research tool for studying MRP4-mediated transport and chemoresistance.
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| Molecular Formula |
C11H10N4S3
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|---|---|
| Molecular Weight |
294.4
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| Exact Mass |
294.006
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| CAS # |
315702-40-0
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| PubChem CID |
704306
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
422.1±55.0 °C at 760 mmHg
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| Flash Point |
209.1±31.5 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.827
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| LogP |
1.85
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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 |
3
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| Heavy Atom Count |
18
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| Complexity |
373
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C(=NNC1=S)CSC2=NC3=CC=CC=C3S2
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| InChi Key |
KVNBVHCJAUXKPJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H10N4S3/c1-15-9(13-14-10(15)16)6-17-11-12-7-4-2-3-5-8(7)18-11/h2-5H,6H2,1H3,(H,14,16)
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| Chemical Name |
3-(1,3-benzothiazol-2-ylsulfanylmethyl)-4-methyl-1H-1,2,4-triazole-5-thione
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| Synonyms |
Ceefourin1; Ceefourin 1; Ceefourin-1
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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 : ~125 mg/mL (~424.56 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 | 3.3967 mL | 16.9837 mL | 33.9674 mL | |
| 5 mM | 0.6793 mL | 3.3967 mL | 6.7935 mL | |
| 10 mM | 0.3397 mL | 1.6984 mL | 3.3967 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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