| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
STAT3 (signal transducer and activator of transcription 3).
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|---|---|
| ln Vitro |
MM-206 is a cell-permeable, non-cytotoxic naphthalene sulfonamide compound that effectively inhibits STAT3 DNA-binding activity with an IC50 of 1.16 µM to 2.45 µM. It inhibits the STAT3 SH2 domain-phosphopeptide interaction with an IC50 of 1.2 µM. The compound displays dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines. MM-206 inhibits G-CSF-stimulated STAT3 signaling. It is a valuable tool for studying STAT3 biology and its role in cancer.
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| ln Vivo |
In vivo efficacy data for MM-206 is limited. The compound is primarily used as an in vitro tool for studying STAT3 biology and its role in cancer. It displays dose-dependent induction of apoptosis in AML cell lines, suggesting potential therapeutic applications in leukemia. Further in vivo studies in xenograft mouse models of AML would be needed to assess its therapeutic potential.
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| Enzyme Assay |
The in vitro enzyme assay for STAT3 DNA-binding inhibition uses a DNA-binding ELISA or electrophoretic mobility shift assay (EMSA). Recombinant STAT3 protein is incubated with a biotinylated DNA probe containing the STAT3 consensus binding sequence and varying concentrations of MM-206 (typically 0.01 to 100 µM). STAT3-DNA complexes are captured on streptavidin-coated plates (for ELISA) or resolved on native polyacrylamide gels (for EMSA). The IC50 for inhibition of DNA binding is calculated from dose-response curves. For SH2 domain binding, a fluorescence polarization assay using a labeled phosphopeptide is performed.
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| Cell Assay |
In vitro cellular assays are performed using acute myeloid leukemia (AML) cell lines or other cancer cell lines with activated STAT3 signaling. Cells are treated with MM-206 at concentrations ranging from 0.01 to 100 µM for 24-72 hours. STAT3 DNA-binding activity is measured using a DNA-binding ELISA or by chromatin immunoprecipitation (ChIP). STAT3 target gene expression (e.g., Bcl-2, Mcl-1, Cyclin D1) is measured by qRT-PCR or Western blot. Apoptosis is assessed by Annexin V/PI staining and flow cytometry, or by measuring caspase-3/7 activity. Cell proliferation is measured using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal model data for MM-206 is not extensively reported in the literature. As a research tool for studying STAT3 biology in cancer, the compound would typically be evaluated in mouse xenograft models using AML or other cancer cell lines with activated STAT3 signaling. Standard efficacy studies would involve compound administration (oral or intraperitoneal) followed by assessment of tumor growth inhibition, STAT3 target gene expression, and apoptosis markers. Pharmacokinetic studies would assess oral bioavailability, plasma half-life, and tissue distribution.
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| ADME/Pharmacokinetics |
MM-206 has a molecular weight of approximately 490 g/mol and is a naphthalene sulfonamide compound. It is cell-permeable and non-cytotoxic. The compound is soluble in DMSO and should be stored as a powder at -20°C. Pharmacokinetic parameters such as oral bioavailability, plasma half-life, and tissue distribution are not extensively characterized in publicly available literature. As a research compound, it is typically used in in vitro assays at concentrations ranging from nanomolar to low micromolar.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for MM-206. The compound is reported to be non-cytotoxic, suggesting a favorable safety profile in vitro. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments for STAT3 inhibitors would typically include selectivity profiling against a panel of transcription factors and kinases to assess off-target effects, hERG channel inhibition for cardiac safety, and CYP450 enzyme inhibition for drug-drug interaction potential.
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| References | |
| Additional Infomation |
MM-206 is a research-grade STAT3 inhibitor that inhibits STAT3 DNA-binding activity and SH2 domain-phosphopeptide interaction. It is not approved for clinical use. The compound is cell-permeable, non-cytotoxic, and displays dose-dependent induction of apoptosis in AML cell lines. MM-206 inhibits G-CSF-stimulated STAT3 signaling. It is supplied as a solid with high purity and should be stored desiccated at -20°C.
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| Molecular Formula |
C22H12F5NO3S2
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|---|---|
| Molecular Weight |
497.45
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| Exact Mass |
497.017
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| CAS # |
1809581-87-0
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| PubChem CID |
102514675
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
601.9±65.0 °C at 760 mmHg
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| Flash Point |
317.8±34.3 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.694
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| LogP |
5.81
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
750
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)SC2=C(C3=CC=CC=C3C(=C2)NS(=O)(=O)C4=C(C(=C(C(=C4F)F)F)F)F)O
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| InChi Key |
ZXJHEANDHXHGMV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H12F5NO3S2/c23-16-17(24)19(26)22(20(27)18(16)25)33(30,31)28-14-10-15(32-11-6-2-1-3-7-11)21(29)13-9-5-4-8-12(13)14/h1-10,28-29H
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| Chemical Name |
2,3,4,5,6-pentafluoro-N-(4-hydroxy-3-phenylsulfanylnaphthalen-1-yl)benzenesulfonamide
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| Synonyms |
MM206; MM-206; MM-206
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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 | 2.0103 mL | 10.0513 mL | 20.1025 mL | |
| 5 mM | 0.4021 mL | 2.0103 mL | 4.0205 mL | |
| 10 mM | 0.2010 mL | 1.0051 mL | 2.0103 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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