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| 25mg |
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Purity: ≥98%
| Targets |
Clanfenur targets the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, thereby preventing tumor cell replication. It also exhibits a wide array of bioactivities, including inhibition of TGF-β and inhibition of human tyrosyl-DNA phosphodiesterase 1 (TDP1). By binding to β-tubulin, it disrupts the mitotic spindle, leading to cell cycle arrest and apoptosis.
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| ln Vitro |
In vitro, Clanfenur demonstrates significant antiproliferative activity against various cancer cell lines. It binds to the colchicine-binding site on β-tubulin, preventing microtubule polymerization and thus tumor cell replication. Its activity as a microtubule inhibitor is consistent with its potential as an antineoplastic agent.
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| ln Vivo |
In vivo, Clanfenur shows antitumor activity. As a substituted benzoylphenylurea, it possesses potential anticancer activity. Its ability to inhibit microtubule polymerization translates to in vivo efficacy in preventing tumor growth.
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| Enzyme Assay |
Clanfenur is evaluated in cell-free assays to measure its binding to tubulin. The compound is incubated with purified tubulin, and the inhibition of polymerization is measured using spectrophotometric methods. Its binding to the colchicine-binding site is assessed using competitive binding assays with radiolabeled colchicine.
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| Cell Assay |
Clanfenur is assessed in cell-based assays using various cancer cell lines. Cells are treated with Clanfenur, and cell proliferation, cell cycle progression, and apoptosis are measured. The compound's ability to inhibit microtubule polymerization and disrupt the mitotic spindle is evaluated using immunofluorescence microscopy.
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| Animal Protocol |
Clanfenur is administered in animal models to evaluate its antitumor efficacy. It has been studied in xenograft models of human cancers. Efficacy is assessed by measuring tumor growth inhibition and survival. The compound is typically formulated for in vivo administration using DMSO or other suitable vehicles.
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| ADME/Pharmacokinetics |
Clanfenur has a molecular weight of 335.08 and a molecular formula of C16H15ClFN3O2. It has a CAS number of 51213-99-1 and a UNII code of KAM54NKT1Q. The compound is a white to off-white solid powder with a purity of ≥98%. It is soluble in DMSO and should be stored at -20°C for up to 3 years.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Clanfenur beyond its preclinical profile. The compound is for research use only and is not intended for human therapeutic use. Its safety profile has not been extensively characterized.
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| References |
Sluiter C, Kettenes-van den Bosch JJ, Hop E, van der Houwen OA, Underberg WJ,
Bult A. Degradation study of the investigational anticancer drug clanfenur. Int J
Pharm. 1999 Aug 20;185(2):227-35. PubMed PMID: 10460918.
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| Additional Infomation |
Clanfenur is a substituted benzoyl urea compound, an analogue of the insecticide difluorophenylurea, and possesses potential antitumor activity. After administration, Clanfenur binds to the colchicine binding site on β-tubulin, inhibiting microtubule polymerization and thus preventing tumor cell replication.
Clanfenur is an investigational anticancer drug that was studied in the 1990s. It is a substituted benzoyl urea compound and an analogue of the insecticide difluorophenylurea. The compound is not approved for clinical use. |
| Molecular Formula |
C5H6N2O2S
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|---|---|
| Molecular Weight |
158.17834
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| Exact Mass |
335.084
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| CAS # |
51213-99-1
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| Related CAS # |
51213-99-1;
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| PubChem CID |
68684
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| Appearance |
White to off-white solid powder
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| Density |
1.371g/cm3
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| Index of Refraction |
1.64
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| LogP |
3.97
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
428
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)C1=C(C(=CC=C1)F)C(=O)NC(=O)NC2=CC=C(C=C2)Cl
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| InChi Key |
SRLPZQAEBMZCIJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15ClFN3O2/c1-21(2)13-5-3-4-12(18)14(13)15(22)20-16(23)19-11-8-6-10(17)7-9-11/h3-9H,1-2H3,(H2,19,20,22,23)
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| Chemical Name |
N-[(4-chlorophenyl)carbamoyl]-2-(dimethylamino)-6-fluorobenzamide
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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 | 6.3219 mL | 31.6096 mL | 63.2191 mL | |
| 5 mM | 1.2644 mL | 6.3219 mL | 12.6438 mL | |
| 10 mM | 0.6322 mL | 3.1610 mL | 6.3219 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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