| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
CFM-4 targets the CARP-1 (Cell division cycle and apoptosis regulator protein 1) and APC-2 (Anaphase-promoting complex subunit 2) protein-protein interaction. By preventing CARP-1 binding to APC-2, CFM-4 disrupts the normal function of the anaphase-promoting complex, a key regulator of the cell cycle. This interference leads to G2/M cell cycle arrest, preventing cancer cells from completing mitosis. CFM-4 also functions as a selective inhibitor of protein kinase CK1δ (Casein Kinase 1 delta).
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| ln Vitro |
In vitro, CFM-4 demonstrates potent activity with an IC₅₀ range of 10-15 μM for CARP-1/APC-2 binding inhibition. It effectively suppresses the growth of drug-resistant human breast cancer cells and tumor cells. The compound enhances CARP-1 expression and induces G2/M cell cycle arrest. CFM-4 has a purity of ≥99.0% and is soluble in DMSO. Specific in vivo efficacy data for CFM-4 are not extensively documented in the available literature. As a research compound targeting cell cycle regulation and apoptosis, it is being investigated for its potential anticancer activity. The compound's ability to inhibit drug-resistant breast cancer cell growth suggests promising in vivo potential that requires further preclinical evaluation.
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| Enzyme Assay |
CARP-1/APC-2 binding inhibition assays are performed using biochemical methods to measure the disruption of protein-protein interactions. CFM-4 is tested at various concentrations, and IC₅₀ values are calculated from dose-response curves. Kinase inhibition assays for CK1δ are conducted using purified enzyme and appropriate substrates. Radiolabeled or fluorescence-based detection methods are used to quantify binding inhibition and enzyme activity.
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| Cell Assay |
Cancer cell lines, particularly drug-resistant human breast cancer cells, are used for in vitro cellular assays. Cells are cultured in appropriate media with 10% FBS at 37°C in 5% CO₂. CFM-4 is dissolved in DMSO and diluted to various concentrations. Cells are treated with CFM-4 and incubated for specified time periods. Cell cycle analysis is performed by flow cytometry using propidium iodide staining. Apoptosis is assessed by Annexin V staining or caspase activity assays. Cell viability is measured by MTT or similar assays.
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| Animal Protocol |
In vivo animal studies are conducted in murine xenograft models using drug-resistant breast cancer cells. CFM-4 is typically administered intraperitoneally or orally. Tumor growth is monitored by caliper measurements. Endpoints include tumor volume, tumor weight, and survival. Histological analysis of tumor tissues is performed to assess apoptosis and cell cycle arrest. Pharmacokinetic and toxicity studies may be conducted to support efficacy evaluations.
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| ADME/Pharmacokinetics |
CFM-4 has a molecular weight of 405.9 and molecular formula C₂₂H₁₆ClN₃OS with CAS number 331458-02-7. It should be stored under recommended conditions as specified in the Certificate of Analysis. The compound is typically shipped on ice packs. For in vivo studies, working solutions should be prepared fresh daily. DMSO solutions should be prepared using freshly opened DMSO as moisture significantly affects solubility.
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| Toxicity/Toxicokinetics |
Specific toxicity data for CFM-4 are not extensively documented in the available literature. As a research compound targeting cell cycle regulation, its safety profile is still being characterized. Standard laboratory safety precautions should be followed when handling this compound. It is intended for research use only and not for human therapeutic applications. The compound should be handled in a well-ventilated area with appropriate personal protective equipment.
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| Additional Infomation |
CFM-4 is a research compound targeting the CARP-1/APC-2 protein-protein interaction with potential applications in cancer research. By inducing G2/M cell cycle arrest and apoptosis, it represents a novel approach to overcoming drug resistance in breast cancer. The compound is commercially available for research purposes only. Its mechanism of action through disruption of the anaphase-promoting complex function makes it a valuable tool for studying cell cycle regulation and apoptosis in cancer biology. Further research is needed to fully characterize its therapeutic potential.
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| Molecular Formula |
C22H16CLN3OS
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|---|---|
| Molecular Weight |
405.9
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| Exact Mass |
405.07
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| CAS # |
331458-02-7
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| PubChem CID |
2871439
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.567
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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 |
28
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| Complexity |
637
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=[N+](C1=CC=C(C2=NNC(=O)CC3=CC(=C(C=C23)OC)OC)C=C1)[O-]
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| InChi Key |
PMADITKBVODKSF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H16ClN3OS/c23-18-12-6-4-10-16(18)14-26-19-13-7-5-11-17(19)22(21(26)27)25-24-20(28-22)15-8-2-1-3-9-15/h1-13,25H,14H2
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| Chemical Name |
1'-[(2-chlorophenyl)methyl]-5-phenylspiro[3H-1,3,4-thiadiazole-2,3'-indole]-2'-one
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| Synonyms |
CFM4; CFM 4; CFM-4
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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 : ~25 mg/mL (~61.59 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 | 2.4637 mL | 12.3183 mL | 24.6366 mL | |
| 5 mM | 0.4927 mL | 2.4637 mL | 4.9273 mL | |
| 10 mM | 0.2464 mL | 1.2318 mL | 2.4637 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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