| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
MM 11253 selectively targets retinoic acid receptor gamma (RARγ), a nuclear receptor that regulates gene expression in response to retinoic acid. It acts as an antagonist, blocking RARγ-mediated transcriptional activity.
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|---|---|
| ln Vitro |
The capacity of MM11389 and MM11254 to stop squamous cell carcinoma cells from growing is blocked by MM11253 [2].
In vitro, MM 11253 potently inhibits RARγ with an IC50 of 44 nM. It has low inhibitory activity against RARα, RARβ, and RXRα, demonstrating high selectivity for RARγ. It blocks the growth-inhibitory effects of RARγ-selective agonists in squamous cell carcinoma (SCC-25) cells. |
| ln Vivo |
In vivo studies for MM 11253 are limited. As a research tool, it is used to study the role of RARγ in development and disease. Detailed in vivo efficacy data have not been published.
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| Enzyme Assay |
The in vitro receptor binding or functional assay for MM 11253 involves measuring its ability to inhibit RARγ-mediated transcriptional activity. A reporter gene assay is typically used, where cells are transfected with a luciferase reporter gene under the control of a retinoic acid response element (RARE) and treated with a RARγ agonist in the presence of MM 11253. The IC50 is determined by measuring luciferase activity.
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| Cell Assay |
Cellular assays for MM 11253 involve treating cells expressing RARγ with the compound and assessing its effect on RARγ target gene expression. The inhibition of RARγ agonist-induced growth inhibition in SCC-25 cells is also measured.
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| Animal Protocol |
In vivo animal studies for MM 11253 are not well-documented. As a research compound, it may be evaluated in animal models of cancer or development, but specific protocols have not been published.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MM 11253 have not been extensively characterized. It has a molecular weight of 462.67 g/mol and a molecular formula of C28H30O2S2.
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| Toxicity/Toxicokinetics |
Toxicity data for MM 11253 are limited. It is a research-grade compound, and comprehensive toxicological evaluations have not been published.
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| References |
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| Additional Infomation |
MM 11253 is a research compound for studying RARγ biology. It has not entered clinical trials. Its mechanism involves selective antagonism of RARγ, making it a valuable tool for investigating the role of RARγ in development, differentiation, and cancer.
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| Molecular Formula |
C28H30O2S2
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|---|---|
| Molecular Weight |
462.67
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| Exact Mass |
462.169
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| CAS # |
345952-44-5
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| PubChem CID |
10389639
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
7.568
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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 |
32
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| Complexity |
710
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DPVGXUNWCVEIGT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H30O2S2/c1-26(2)11-12-27(3,4)24-17-22(9-10-23(24)26)28(31-13-14-32-28)21-8-7-18-15-20(25(29)30)6-5-19(18)16-21/h5-10,15-17H,11-14H2,1-4H3,(H,29,30)
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| Chemical Name |
6-[2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-1,3-dithiolan-2-yl]naphthalene-2-carboxylic acid
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| Synonyms |
MM11253; MM-11253; MM 11253
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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 (~270.17 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 | 2.1614 mL | 10.8068 mL | 21.6137 mL | |
| 5 mM | 0.4323 mL | 2.1614 mL | 4.3227 mL | |
| 10 mM | 0.2161 mL | 1.0807 mL | 2.1614 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.