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STAT3-IN-1 is a novel, oral and selective STAT3 inhibitor with anticancer activity. It inhibits STAT3 with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively.It can induce tumor apoptosis.
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| ln Vitro |
Compound 7d, STAT3-IN-1, suppresses the acetylation of STAT3 lysine 685 and modifies the expression of its specific gene [1]. In MDA-MB-231 cells, STAT3-IN-1 (compound 7d: 0-10 μM, 48 h) causes tumor cell death [1].
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| ln Vivo |
In a mouse xenograft model, STAT3-IN-1 (Compound 7d: 10, 20 mg/kg, two weeks) inhibits tumor growth with minimal toxicity [1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: MDA-MB-231 cell lines. Tested Concentrations: 0-10 μM. Incubation Duration: 48 hrs (hours). Experimental Results: The induced apoptosis rates (early and late apoptosis) at 1, 2, 5, 8 and 10 μM were 9.0%, 11.2%, 20.9%, 43.3% and 85.2% versus control 3.0%. Western Blot Analysis[1] Cell Types: MDA-MB-231 and HT-29 cell lines. Tested Concentrations: 0-10 μM. Incubation Duration: 48 hrs (hours). Experimental Results: Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells. Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1), CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685. |
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| Animal Protocol |
Animal/Disease Models: Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells[1].
Doses: 10, 20 mg/kg. Route of Administration: Oral administration once every other day for two weeks. Experimental Results: Arrested tumor growth with no obvious body weight loss. |
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| References |
[1]. Li S, et al. Discovery of oral-available resveratrol-caffeic acid based hybrids inhibiting acetylated and phosphorylated STAT3 protein. Eur J Med Chem. 2016 Nov 29;124:1006-1018.
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| Molecular Formula |
C₂₈H₂₉NO₆
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|---|---|
| Molecular Weight |
475.53
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| CAS # |
2059952-75-7
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| SMILES |
O=C(NC1=CC=C(/C=C/C2=CC(OC)=CC(OC)=C2)C=C1)/C=C/C3=CC(OC)=C(OC)C(OC)=C3
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| InChi Key |
KOZAEBHIXYBHKA-FCXQYMQBSA-N
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| InChi Code |
InChI=1S/C28H29NO6/c1-31-23-14-20(15-24(18-23)32-2)7-6-19-8-11-22(12-9-19)29-27(30)13-10-21-16-25(33-3)28(35-5)26(17-21)34-4/h6-18H,1-5H3,(H,29,30)/b7-6+,13-10+
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| Chemical Name |
(E)-N-(4-((E)-3,5-dimethoxystyryl)phenyl)-3-(3,4,5-trimethoxyphenyl)acrylamide
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| Synonyms |
STAT3-IN 1 STAT3 IN-1 STAT3-IN1STAT3IN1 STAT3 IN 1STAT3-IN-1 STAT3IN-1 STAT3-IN-compound 7d
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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 (~262.86 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 6.25 mg/mL (13.14 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (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 62.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1029 mL | 10.5146 mL | 21.0292 mL | |
| 5 mM | 0.4206 mL | 2.1029 mL | 4.2058 mL | |
| 10 mM | 0.2103 mL | 1.0515 mL | 2.1029 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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