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| Targets |
STAT3-IN-11 directly targets the STAT3 protein. It inhibits the phosphorylation of STAT3 at the critical Tyr705 residue. This action prevents the activation and nuclear translocation of STAT3, thereby blocking its function as a transcription factor. As a result, the transcription of downstream target genes like Survivin and Mcl-1 is reduced. It does not affect upstream tyrosine kinases like Src and JAK2, nor does it affect p-STAT1.
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| ln Vitro |
On MDA-MB-231 cells, STAT3-IN-11 (20 μM, 48 h) had a 97.86% inhibitory impact [1]. At IC50 values of 6.01 μM (MDA-MB-231) and 7.02 μM (HepG2, A549), STAT3-IN-11 (0-30 μM, 48 h) inhibits a range of cancer cells, whereas at IC50 values of 26.54 μM (MDA-MB-10A), 26.69 μM (PBMC), and 12.52 μM (HFL-1) it inhibits normal human cells [1]. The phosphorylation of STAT3 (induced by IL-6 in MDA-MB-231) at pTyr705 is dose-dependently inhibited by STAT3-IN-11 (2.5-10 μM, 6 hours) [1]. In a concentration-dependent manner, STAT3-IN-11 (2.5-10 μM, 6 h) suppresses the expression of STAT3 downstream genes, namely Mcl-1 and Survivin [1]. The phosphorylation of canonical upstream kinases of STAT3 (p-JAK2 and p-Src) and STAT1 (a STAT isoform) is unaffected by STAT3-IN-11 (2.5–10 μM, 6 hours) [1]. Apoptosis can be induced dose-wise by STAT3-IN-11 (2.5-10 μM, 48 h) [1].
In vitro, STAT3-IN-11 dose-dependently inhibits the IL-6-stimulated phosphorylation of STAT3 at the pTyr705 site in MDA-MB-231 cells (2.5-10 μM, 6 hours). It inhibits the phosphorylation of downstream genes Survivin and Mcl-1. This leads to the induction of cancer cell apoptosis. Its anti-proliferative activity has been demonstrated in cancer cell models. |
| ln Vivo |
In vivo activity data for STAT3-IN-11 are not extensively detailed in standard product descriptions, but as a selective STAT3 inhibitor that promotes apoptosis in cancer cells, it is considered a promising candidate for anti-tumor research. Its in vivo efficacy would be expected to be evaluated in relevant animal models of cancer.
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| Enzyme Assay |
The primary non-cellular assay for STAT3-IN-11 involves measuring its binding affinity to the STAT3 protein. This is typically performed using a fluorescence polarization (FP) or surface plasmon resonance (SPR) assay where the compound competes with a labeled probe for binding to the STAT3 protein. The IC50 or Kd value is determined from the competition curve.
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| Cell Assay |
Cytotoxicity assay [1]
Cell Types: MDA-MB-231 Cell Tested Concentrations: 20 μM Incubation Duration: 48 hrs (hours) Experimental Results: Anti-proliferative activity reached 97.86%. Cytotoxicity assay[1] Cell Types: MDA-MB231, A549, MDA-MB-10A, PBMC and HFL-1 Cell Tested Concentrations: 20 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition with IC50 values of 6.01, 7.20, 7.02, 26.54 25.69 and 12.52 μM for MDA-MB231, A549, MDA-MB-10A, PBMC and HFL-1 cells, respectively. Western Blot Analysis[1] Cell Types: MDA-MB-231 Cell Tested Concentrations: 2.5, 5 and 10 μM Incubation Duration: 6 hrs (hours) Experimental Results: diminished the level of p-STAT3 at pTyr705 site in a concentration-dependent manner. Western Blot Analysis [1] Cell Types: MDA-MB-231 Cell Tested Concentrations: 2.5, 5 and 10 μM Incubation Duration: 6 hrs (hours) Experimental Results: STAT3 downstream gene levels were down-regulated. Apoptosis analysis [1] Cell Types: MDA-MB-231 Cell Tested Concentrations: 5, 10 and 15 μM Incubation Duration: 48 hrs (hours) Experimental Results: At a concentration of 15 μM, the percentage of apoptotic cells was 24.4%. In vitro cellular assays for STAT3-IN-11 commonly use cancer cell lines like MDA-MB-231 (breast cancer). Cells are treated with the compound, often following stimulation with IL-6 to activate the STAT3 pathway. The phosphorylation status of STAT3 (pTyr705) and its downstream targets (Survivin, Mcl-1) is analyzed by Western blotting or ELISA. Apoptosis is quantified using assays like Annexin V/PI staining, and cell viability is assessed via MTT or CellTiter-Glo assays. |
| Animal Protocol |
In vivo animal studies for STAT3-IN-11 are not detailed in standard product information. As a preclinical research compound, its in vivo efficacy and pharmacokinetics would typically be evaluated in xenograft mouse models. Tumor-bearing mice would be administered STAT3-IN-11, and tumor growth inhibition would be monitored as the primary endpoint.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of STAT3-IN-11 are not extensively described. As a small molecule (MW 335.35), it is likely suitable for oral administration. It is soluble in DMSO. Further in vivo studies would be required to fully characterize its absorption, distribution, metabolism, and excretion.
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| Toxicity/Toxicokinetics |
Specific toxicological data for STAT3-IN-11 are not available in standard product documentation. As a research-use compound, comprehensive toxicity profiles are not typically provided. It is intended for research use only and not for human therapeutic use. Standard laboratory safety precautions should be observed.
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| References | |
| Additional Infomation |
STAT3-IN-11 is a research-grade compound for laboratory use only and is not approved for clinical use. Its CAS number is 2503096-50-0, and its molecular formula is C₂₀H₁₇NO₄. Its primary application is in cancer research to study STAT3 signaling, investigate the role of STAT3 in tumorigenesis, and explore the therapeutic potential of STAT3 inhibitors. It is a valuable tool for developing anti-tumor agents targeting the STAT3 pathway.
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| Molecular Formula |
C20H17NO4
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| Molecular Weight |
335.353285551071
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| Exact Mass |
335.115
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| CAS # |
2503096-50-0
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| PubChem CID |
164517204
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| Appearance |
Yellow to orange solid powder
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| LogP |
3.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
589
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(NCCC1=C(C)C(=O)C2=C(C1=O)C(O)=CC=C2)(=O)C1=CC=CC=C1
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| InChi Key |
XLSYRTJOLUDGSR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H17NO4/c1-12-14(10-11-21-20(25)13-6-3-2-4-7-13)19(24)17-15(18(12)23)8-5-9-16(17)22/h2-9,22H,10-11H2,1H3,(H,21,25)
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| Chemical Name |
N-[2-(8-hydroxy-3-methyl-1,4-dioxonaphthalen-2-yl)ethyl]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) |
DMSO : ~100 mg/mL (~298.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.45 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9820 mL | 14.9098 mL | 29.8196 mL | |
| 5 mM | 0.5964 mL | 2.9820 mL | 5.9639 mL | |
| 10 mM | 0.2982 mL | 1.4910 mL | 2.9820 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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