| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Stattic (6-Nitro-1-benzothiophene 1,1-dioxide) is a small molecule inhibitor of STAT3 that potently inhibits STAT3 activation and nuclear translocation with potential antineoplastic activity. It inhibits STAT3 with an IC50 of 5.1 μM in cell-free assays, and exhibits high selectivity for STAT3 over STAT1. Stattic is the first nonpeptidic small molecule inhibitor of STAT3 with IC50 values of 2.562 ± 0.409 μM, 3.481 ± 0.953 μM, 2.282 ± 0.423 μM and 2.648 ± 0.542 μM, respectively, in UM-SCC-17B, OSC-19, Cal33 and UM-SCC-22B cell lines. Stattic is reported to selectively inhibit dimerization, activation and nuclear translocation of STAT3. It can also induce the apoptosis of STAT3-dependent breast cancer cell lines.
| ln Vitro |
In the ALDH+ and D44+/CD24+ subpopulations of Panc-1 and HPAC pancreatic cancer cell lines lacking P-ERK1/ 2, stattic (20 μM; 24 hours) preferentially inhibits P-STAT3 and inhibits STAT3 phosphorylation (Y705), as evidenced by the suppression of [1]. In PC3M-1E8 cells, stattic (2.5, 5, 10 μM; 4 hours) dramatically decreased the nuclear levels of survivin and pSTAT3 at 10 μM. A dose-dependent way is observed in the inhibition of IL-6-induced STAT3 activation by Stattic (2.5-10 μM; 24 hours) [2]. PC3M-1E8 cells, which are prostate cancer cells, exhibit growth inhibition and apoptosis in response to stattic (2.5, 5, 10 μM; 48 hours). At 2.5 μM and 5 μM, stattic does not significantly cause apoptosis [2]. Stattic (2.5, 5, 10 μM; 48 hours) exhibits a notable buildup of S-phase [2]. Stattic leads in very low levels of STAT3 phosphorylation and neither major morphological alterations nor apoptosis in A2780 cells or HUVEC cells [2].
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| ln Vivo |
In Alport syndrome (AS) mice, stattic (10 mg/kg; intraperitoneal injection; three times a week for ten weeks) improves renal dysfunction [3].
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| Animal Protocol |
Animal/Disease Models: Age-matched wild-type (WT) C57BL/6 mice[3]
Doses: 10 mg/kg Route of Administration: IP; three timesper week for 10 week Experimental Results: Increased levels of proteinuria, BUN and serum creatinine. Dramatically suppressed the gene expression levels of renal injury markers (Lcn2, Kim-1), pro-inflammatory cytokines (Il-6, KC), pro-fibrotic genes (Tgf-β, Col1a1, α-Sma) and Mmp9. |
| References | |
| Additional Infomation |
Stattic is a member of the class of 1-benzothiophenes that is 1-benzothiophene-1,1-dioxide substituted at position 6 by a nitro group. Used as a radiosensitising agent for esophageal squamous cell carcinoma. It has a role as an antineoplastic agent, a STAT3 inhibitor and a radiosensitizing agent. It is a member of 1-benzothiophenes, a C-nitro compound and a sulfone.
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| Molecular Formula |
C8H5NO4S
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|---|---|---|
| Molecular Weight |
211.19
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| Exact Mass |
210.993
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| CAS # |
19983-44-9
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| Related CAS # |
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| PubChem CID |
2779853
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
461.1±45.0 °C at 760 mmHg
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| Melting Point |
184ºC
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| Flash Point |
232.6±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.671
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| LogP |
1.31
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
14
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| Complexity |
375
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZRRGOUHITGRLBA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H5NO4S/c10-9(11)7-2-1-6-3-4-14(12,13)8(6)5-7/h1-5H
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| Chemical Name |
6-nitro-1-benzothiophene 1,1-dioxide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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. View More
Solubility in Formulation 3: 2% DMSO +30%PEG 300 +H2O:8 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7351 mL | 23.6754 mL | 47.3507 mL | |
| 5 mM | 0.9470 mL | 4.7351 mL | 9.4701 mL | |
| 10 mM | 0.4735 mL | 2.3675 mL | 4.7351 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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