| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
STAT3
STAT3-IN-17 targets STAT3, a transcription factor that plays a critical role in cell proliferation, survival, and immune regulation. It inhibits STAT3 activity with an IC50 of 0.7 μM as measured in HEK-Blue IL-6 cells, a cell-based assay that reports on STAT3-dependent transcriptional activation. By blocking STAT3 signaling, the compound reduces the expression of downstream target genes involved in tumor growth, angiogenesis, and immunosuppression, making it a useful tool for studying STAT3 biology. |
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| ln Vitro |
STAT3-IN-17 (Compound 15) (10 μM; 20 h, 48 h) inhibits the STAT3 pathway at a rate of 76.5% and reduces the viability of HEK-Blue IL-6 cells to 15%[1]. STAT3 phosphorylation (Y705) is inhibited by STAT3-IN-17 (2.5–40 μM; 24 h)[1]. With an IC50 value of 2.7 μM, STAT3-IN-17 (10 μM, 50 μM; 48 h) suppresses the development of HeLa and HEK 293T cells[1]. The bacteria Helicobacter pylori and Campylobacter jejuni are inhibited by (D)-PPA 1 (compound 24), with MIC values of 1.6 μM and 4.7 μM, respectively [2].
STAT3-IN-17 demonstrates moderate STAT3 inhibitory activity with an IC50 of 0.7 μM in HEK-Blue IL-6 cells. It exhibits antiproliferative activity in HeLa cells, indicating its potential to suppress cancer cell growth. The compound is used in various in vitro assays to evaluate STAT3-dependent signaling pathways and to study the effects of STAT3 inhibition on tumor cell proliferation and survival. Its moderate potency makes it a useful tool for proof-of-concept studies. |
| ln Vivo |
In rats, STAT3-IN-17 (Compound 15) (5 mg/kg gavage or 25 mg/kg intravenously; single dose) demonstrates superior pharmacokinetic properties compared to nitazoxanide. Its elimination half-life (t1/2β) is significantly longer (11.1 vs 0.8 h), its absolute bioavailability (F) is higher (87.4% vs 5.7%), and its maximum plasma concentration (Cmax) is higher (20.7 vs 1.0 mg/L)[1].
In vivo activity data for STAT3-IN-17 are not extensively reported. The compound has good pharmacokinetic characteristics, suggesting potential for in vivo applications. It is primarily used as a research tool for studying STAT3 signaling in cellular models. Further research is needed to characterize its efficacy in animal models of cancer and inflammation. The compound's moderate potency and favorable PK properties may make it a candidate for further optimization and in vivo evaluation. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for STAT3-IN-17 typically involves a STAT3 DNA-binding assay or a STAT3 phosphorylation assay. In a typical setup, recombinant STAT3 protein or nuclear extracts from STAT3-activated cells are incubated with a biotinylated DNA probe containing a STAT3 consensus binding sequence. The compound's ability to inhibit STAT3-DNA binding is measured using an ELISA-based or electrophoretic mobility shift assay (EMSA). Alternatively, a TR-FRET assay using labeled STAT3 and a phosphopeptide probe can be employed to measure SH2 domain binding.
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| Cell Assay |
The in vitro cellular assay for STAT3-IN-17 typically uses HEK-Blue IL-6 cells, which are engineered to express a STAT3-inducible secreted alkaline phosphatase (SEAP) reporter. Cells are treated with varying concentrations of the compound and stimulated with IL-6 to activate STAT3. SEAP activity in the culture supernatant is then measured to quantify STAT3-dependent transcriptional activity, from which the IC50 is calculated. Antiproliferative activity is assessed in HeLa cells using standard cell viability assays such as MTT or CellTiter-Glo.
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| Animal Protocol |
In vivo animal studies for STAT3-IN-17 are not extensively documented. Given its good pharmacokinetic characteristics, potential in vivo models include xenograft tumor models in mice, where tumor growth inhibition and STAT3 phosphorylation levels are assessed following administration of the compound. However, specific protocols for STAT3-IN-17 in animal models have not been reported in the available literature. Researchers should design appropriate experiments based on the compound's properties and the biological question being investigated.
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| ADME/Pharmacokinetics |
STAT3-IN-17 has good pharmacokinetic characteristics, making it suitable for further in vivo evaluation. Specific ADME parameters such as half-life, bioavailability, clearance, and volume of distribution are not detailed in the available literature. The compound is soluble in DMSO and can be formulated for various administration routes. Researchers should perform their own pharmacokinetic studies to determine appropriate dosing regimens if in vivo application is intended.
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| Toxicity/Toxicokinetics |
Toxicity data for STAT3-IN-17 are not available in the public domain. As a research compound, comprehensive toxicological evaluations have not been performed. The compound is intended for laboratory research use only and should be handled with standard safety precautions. Appropriate personal protective equipment should be worn when handling this compound. Consult the product's safety data sheet for specific handling and disposal instructions.
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| References | |
| Additional Infomation |
STAT3-IN-17 is a moderate STAT3 inhibitor (IC50 = 0.7 μM) with antiproliferative activity in HeLa cells and good pharmacokinetic characteristics. It is used in oncology and immunology research to study STAT3-dependent signaling pathways and therapeutic strategies. The compound serves as a chemical probe for investigating tumor growth and inflammatory microenvironment modulation. STAT3-IN-17 is not in clinical trials and has not been approved for therapeutic use. It remains an experimental tool for basic research into STAT3 biology.
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| Molecular Formula |
C11H6F3N3O3S
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|---|---|
| Molecular Weight |
317.2439
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| Exact Mass |
317.008
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| CAS # |
1245814-52-1
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| PubChem CID |
129396559
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
408
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(=C([H])N=C1N([H])C(C1C([H])=C([H])C(C(F)(F)F)=C([H])C=1[H])=O)[N+](=O)[O-]
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| InChi Key |
HKCGJKNZQDBZFT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H6F3N3O3S/c12-11(13,14)7-3-1-6(2-4-7)9(18)16-10-15-5-8(21-10)17(19)20/h1-5H,(H,15,16,18)
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| Chemical Name |
N-(5-nitro-1,3-thiazol-2-yl)-4-(trifluoromethyl)benzamide
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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 | 3.1522 mL | 15.7609 mL | 31.5219 mL | |
| 5 mM | 0.6304 mL | 3.1522 mL | 6.3044 mL | |
| 10 mM | 0.3152 mL | 1.5761 mL | 3.1522 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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