| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
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| Targets |
CD 2314 targets the retinoic acid receptor beta (RARβ), a nuclear receptor that regulates gene transcription in response to retinoic acid. RARβ is involved in cell differentiation, proliferation, and apoptosis. Selective activation of RARβ by CD 2314 makes it a valuable tool for studying RARβ-mediated biological processes.
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| ln Vitro |
In vitro, CD 2314 inhibits the growth of human head and neck squamous cell carcinoma (HNSCC) 22B, 183A, and 22A cells with IC50 values of 3.0, 5.7, and 8.0 μM, respectively. It demonstrates potent and selective RARβ agonism with a Kd of 145 nM for RARβ and >3760 nM for RARα, with no binding detected at RARγ.
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| ln Vivo |
In vivo, CD 2314 has been studied for its effects on RARβ-mediated gene expression and tumor growth inhibition. As a selective RARβ agonist, it may induce differentiation and apoptosis in RARβ-expressing tumors. Specific in vivo data including dose-response relationships and efficacy in tumor models are available from published studies.
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| Enzyme Assay |
In vitro receptor binding assays for RARβ agonists typically use radioligand binding with [³H]all-trans-retinoic acid (ATRA) as the labeled ligand. Membranes prepared from cells expressing RARβ, RARα, or RARγ are incubated with the radioligand and varying concentrations of CD 2314. Specific binding is determined by subtracting non-specific binding. Kd values are calculated from saturation or competition binding curves.
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| Cell Assay |
In vitro cellular assays for RARβ agonists typically use cancer cell lines expressing RARβ, such as HNSCC cells. Cells are treated with CD 2314 at various concentrations, and cell viability is measured using MTT or CCK-8 assays. IC50 values for growth inhibition are calculated from dose-response curves. RARβ-mediated gene expression can be measured by qRT-PCR or reporter gene assays.
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| Animal Protocol |
In vivo animal studies for RARβ agonists typically use xenograft tumor models in immunocompromised mice. Animals are implanted with RARβ-expressing tumor cells and treated with CD 2314 at various doses via oral or intraperitoneal administration. Tumor growth is monitored by caliper measurement, and tumor weight is determined at study termination. RARβ target gene expression is assessed in tumor tissue.
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| ADME/Pharmacokinetics |
CD 2314 is a small-molecule RARβ agonist with physicochemical properties suitable for oral administration. It is expected to have good bioavailability and tissue distribution. The compound is metabolized in the liver, and its metabolites are excreted via the kidneys and bile. Detailed PK parameters are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CD 2314 would typically include acute and repeated-dose toxicity in rodents, as well as genotoxicity and safety pharmacology assessments. As a retinoid receptor agonist, potential side effects may include skin irritation, mucocutaneous effects, and teratogenicity, which are class effects of retinoids.
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| References | |
| Additional Infomation |
CD 2314 is a potent and selective RARβ receptor agonist with a Kd of 145 nM for RARβ and no binding at RARγ. It inhibits the growth of human HNSCC cells with IC50 values ranging from 3.0 to 8.0 μM. The compound is a valuable research tool for studying RARβ-mediated biology and is available for research use only.
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| Molecular Formula |
C23H24O2S
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|---|---|
| Molecular Weight |
364.5
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| Exact Mass |
364.15
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| CAS # |
170355-37-0
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| PubChem CID |
15293210
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| Appearance |
White to light yellow solid powder
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| LogP |
6.615
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
URUSABQSUCBGGJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24O2S/c1-22(2)7-8-23(3,4)19-11-16-9-15(6-5-14(16)10-18(19)22)20-12-17(13-26-20)21(24)25/h5-6,9-13H,7-8H2,1-4H3,(H,24,25)
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| Chemical Name |
5-(5,5,8,8-tetramethyl-6,7-dihydroanthracen-2-yl)thiophene-3-carboxylic acid
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| Synonyms |
CD-2314; CD 2314; CD2314
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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 | 2.7435 mL | 13.7174 mL | 27.4348 mL | |
| 5 mM | 0.5487 mL | 2.7435 mL | 5.4870 mL | |
| 10 mM | 0.2743 mL | 1.3717 mL | 2.7435 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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