STAT3-SH2 domain inhibitor 1
Based on 1 Customer Validation
STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer.
For research use only. We do not sell to patients.
- Purity: 98.58%
- CAS No.: 2816059-41-1
- Formula: C28H28BF5N2O5S
- Molecular Weight:610.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AGS | IC50 |
1.54 μM
Compound: 7; W1046
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Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human AGS cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36170649] |
| H9c2 | IC50 |
9.05 μM
Compound: 7; W1046
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Antiproliferative activity against human H9c2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human H9c2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 36170649] |
| MGC-803 | IC50 |
4.73 μM
Compound: 7; W1046
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Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay
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[PMID: 36170649] |
STAT3-SH2 domain inhibitor 1 (compound 7; 1-5 μM; 24 h; AGS and MGC-803 cell lines) strongly and selectively inhibits the STAT3 signaling pathway[1].
STAT3-SH2 domain inhibitor 1 (0-10 μM; 72 h) has antiproliferative activity with IC50 values of 1.54 and 4.73 μM for AGS and MGC-803 cells, respectively[1].
STAT3-SH2 domain inhibitor 1 (1 and 3 μM; 72 h; AGS and MGC-803 cell lines) induces apoptosis effects in gastric cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AGS and MGC-803 cell lines
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Concentration:0-10 μM
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Incubation Time:72 hours
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Result:Suppressed cancer cell proliferation and growth.
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Cell Line:AGS and MGC-803 cell lines
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Concentration:1 and 3 μM
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Incubation Time:72 hours
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Result:Induced apoptosis in AGS cells in a concentration-dependent manner, resulting in apoptotic percentages of 13.0 and 26.7% at 1 and 3 μM, respectively.
Induced apoptosis of MGC-803 cells in a dose-dependent way, leading to apoptotic percentage of 11.2% at 5 μM.
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Cell Line:AGS and MGC-803 cell lines
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Concentration:1 and 3 μM
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Incubation Time:24 hours
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Result:Inhibited STAT3 phosphorylation at Tyr705 in a dose-dependent manner.
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Cell Line:HEK-293T cells
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Concentration:1, 3, and 5 μM
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Incubation Time:24 hours
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Result:Disrupted STAT3 dimerization in HEK-293T cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c male nude mice with gastric tumor xenografts[1]
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Dosage:5 and 15 mg/kg
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Administration:Intraperitoneal injection; daily, for 20 days
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Result:Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) of 65.14% at 5 mg/kg and 79.13% at 15 mg/kg, respectively.
Chemical Information
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CAS No. 2816059-41-1
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Appearance Solid
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Molecular Weight 610.40
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Formula C28H28BF5N2O5S
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Color White to off-white
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SMILES
O=C(N(C1=CC=C(B(O)O)C=C1)CC2=CC=C(C3CCCCC3)C=C2)CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 8.33 mg/mL (13.65 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 0.83 mg/mL (1.36 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 0.83 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.83 mg/mL (1.36 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 0.83 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6383 mL | 8.1913 mL | 16.3827 mL | 40.9567 mL |
| 5 mM | 0.3277 mL | 1.6383 mL | 3.2765 mL | 8.1913 mL | |
| 10 mM | 0.1638 mL | 0.8191 mL | 1.6383 mL | 4.0957 mL |
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