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STAT3-IN-13 is a novel and potent STAT3 inhibitor with anticancer activity. STAT3-IN-13 exhits anti-proliferative activity by binding to the STAT3 SH2 domain with a KD of 0.46 μM.
| ln Vitro |
Compound 6f (STAT3-IN-13) has anti-proliferative action against MG63, HOS, and 143B cells, with IC50 values of 0.25, 0.11, and 0.55 μM, respectively, over a 48-hour period[1]. Compound 6f (STAT3-IN-13) exhibits concentration-dependent behavior with a KD of 0.96 μM, as it binds to STAT3 and interacts with STAT3586−685 [1]. Compound 6f, or STAT3-IN-13, reduces STAT3 in tumor cells and inhibits STAT3 Y705 phosphorylation in 143B and HOS cells (0-1.0 μM; 24 hours)[1]. Compound 6f, STAT3-IN-13, promotes apoptosis in 143B cells in a dose-dependent manner (0-1.0 μM; 48 hours)[1].
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| ln Vivo |
Compound 6f, STAT3-IN-13 (10–20 mg/kg; ip; twice daily, for 4 weeks; nude mice), inhibits the growth and metastasis of osteosarcoma in vivo[1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: 143B cells Tested Concentrations: 0, 0.2, 0.5, and 1 μM Incubation Duration: 48 hrs (hours) Experimental Results: Increased the percentage of apoptosis rates of 3.4%, 8.7%, 10.7%, and 23.3% at 0, 0.2, 0.5 and 1 μM, respectively. Western Blot Analysis[1] Cell Types: 143B and HOS cells Tested Concentrations: 0, 0.2, 0.5 and 1.0 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited STAT3 Y705 phosphorylation and downstream target gene expression including Bcl -2 and VEGF, retained good antitumor activities against control tumor cells without STAT3 knockdown. |
| Animal Protocol |
Animal/Disease Models: Nude mice
Doses: 10 and 20 mg/kg Route of Administration: intraperitoneal (ip)injection; twice (two times) daily, for 4 weeks Experimental Results: Suppressed tumor weight at a dose of 10 mg/kg. |
| References |
| Molecular Formula |
C21H20N6O3S
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|---|---|
| Molecular Weight |
436.486902236938
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| Exact Mass |
436.131
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| CAS # |
2248552-86-3
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| PubChem CID |
163358781
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| Appearance |
Yellow to brown solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
721
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1N(C(NC2=CC=C(OC)C=C2)=O)CCC2C(C#N)=C(NC(C3=CN(C)N=C3)=O)SC1=2
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| InChi Key |
WVYHDFDOBCBKGI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H20N6O3S/c1-26-11-13(10-23-26)19(28)25-20-17(9-22)16-7-8-27(12-18(16)31-20)21(29)24-14-3-5-15(30-2)6-4-14/h3-6,10-11H,7-8,12H2,1-2H3,(H,24,29)(H,25,28)
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| Chemical Name |
3-cyano-N-(4-methoxyphenyl)-2-[(1-methylpyrazole-4-carbonyl)amino]-5,7-dihydro-4H-thieno[2,3-c]pyridine-6-carboxamide
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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 | 2.2910 mL | 11.4550 mL | 22.9100 mL | |
| 5 mM | 0.4582 mL | 2.2910 mL | 4.5820 mL | |
| 10 mM | 0.2291 mL | 1.1455 mL | 2.2910 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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