| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 1g | |||
| Other Sizes |
| Targets |
CCT-365623 targets lysyl oxidase (LOX), a copper-dependent amine oxidase that cross-links collagen and elastin in the extracellular matrix. LOX plays a critical role in tumor progression by trapping EGF receptors at the cell surface. By inhibiting LOX, CCT-365623 disrupts this process, leading to anti-metastatic effects. It has a molecular formula of C18H17NO4S3 and a molecular weight of 407.53.
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| ln Vitro |
CCT-365623 is a potent inhibitor of lysyl oxidase (LOX) with an IC50 of 0.9 μM. It is approximately 16-fold more potent than BAPN (IC50 = 14.7 μM). In vitro, the compound effectively inhibits LOX enzymatic activity, disrupting EGFR cell surface retention. This inhibition is associated with its anti-metastatic properties, making it a valuable tool for cancer research.
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| ln Vivo |
CCT-365623 has demonstrated strong anti-metastatic effects in vivo. As an orally bioavailable LOX inhibitor, it shows significant efficacy in preclinical models of cancer metastasis. The compound's ability to inhibit LOX in vivo contributes to its therapeutic potential in preventing tumor spread and progression.
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| Enzyme Assay |
CCT-365623's activity is assessed using in vitro enzyme assays to measure its inhibition of lysyl oxidase (LOX) activity. These assays typically involve incubating the compound with LOX enzyme and a suitable substrate, followed by detection of the enzymatic product. The IC50 value of 0.9 μM is determined from dose-response curves. Selectivity profiling is performed to evaluate its specificity against other related enzymes.
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| Cell Assay |
Cellular assays for CCT-365623 involve treating cancer cells with the compound and assessing its effects on LOX activity, cell migration, and invasion. The compound's ability to inhibit LOX-mediated processes, such as EGFR cell surface retention, can be evaluated using cell-based assays. These studies help elucidate the cellular mechanisms underlying its anti-metastatic activity.
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| Animal Protocol |
In vivo animal model protocols for CCT-365623 involve oral administration to tumor-bearing mice to evaluate its anti-metastatic efficacy. The compound's ability to inhibit tumor progression and metastasis is assessed by measuring tumor growth, metastatic burden, and survival rates. These studies are crucial for validating LOX as a therapeutic target and evaluating the compound's potential for clinical development.
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| ADME/Pharmacokinetics |
CCT-365623 is an orally bioavailable compound with favorable pharmacokinetic properties. It demonstrates good oral bioavailability, supporting its use in in vivo studies. The compound is soluble in DMSO and can be formulated for oral administration. Its pharmacokinetic profile has been characterized to support preclinical efficacy studies.
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| Toxicity/Toxicokinetics |
CCT-365623 is intended for research use only and not for human consumption. As a research compound, its comprehensive toxicological profile may not be fully characterized. However, standard safety assessments would be required for clinical development. The compound is generally well-tolerated in preclinical models at efficacious doses.
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| References |
Lysyl
oxidase drives tumour progression by trapping EGF receptors at the cell surface.
Nat Commun. 2017 Apr 18;8:14909. doi: 10.1038/ncomms14909.
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| Additional Infomation |
CCT-365623 (CAS# 2126134-01-6) is a research compound primarily used to study the role of lysyl oxidase (LOX) in cancer biology. It is not approved for clinical use and is supplied as a solid powder for research purposes. The compound is a potent LOX inhibitor with significant anti-metastatic activity, making it a valuable tool for drug discovery and target validation.
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| Molecular Formula |
C18H17NO4S3
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|---|---|
| Molecular Weight |
407.526880979538
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| Exact Mass |
407.032
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| CAS # |
2126134-01-6
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| Related CAS # |
CCT365623 hydrochloride;2126136-98-7
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| PubChem CID |
130345035
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
674
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ADIBEGOVRYXDOX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17NO4S3/c1-25(20,21)16-9-14(13-5-3-2-4-6-13)10-17(11-16)26(22,23)18-8-7-15(12-19)24-18/h2-11H,12,19H2,1H3
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| Chemical Name |
[5-(3-methylsulfonyl-5-phenylphenyl)sulfonylthiophen-2-yl]methanamine
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| Synonyms |
CCT 365623.CCT365623 CCT-365623
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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 | 2.4538 mL | 12.2690 mL | 24.5381 mL | |
| 5 mM | 0.4908 mL | 2.4538 mL | 4.9076 mL | |
| 10 mM | 0.2454 mL | 1.2269 mL | 2.4538 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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