SI-109
Based on 2 publication(s) in Google Scholar
SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.
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- Purity: 98.96%
- CAS No.: 2429877-30-3
- 화학식: C40H44F2N7O9P
- 분자량:835.79
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보관:
-80°C, stored under nitrogen
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SI-109
More
Biological Activity
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STAT3 9 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SU-DHL-1 | IC50 |
>10 μM
Compound: 8; SI-109
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Antiproliferative activity against human SUDHL1 cells assessed as reduction in cell viability incubated for 4 days by cell-titer glo luminescent assay
Antiproliferative activity against human SUDHL1 cells assessed as reduction in cell viability incubated for 4 days by cell-titer glo luminescent assay
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[PMID: 31747516] |
| SU-DHL-1 | IC50 |
>10 μM
Compound: SI-109
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Antiproliferative activity against human SU-DHL-1 cells assessed as cell growth inhibition incubated for 4 days by CellTiter-Glo asssay
Antiproliferative activity against human SU-DHL-1 cells assessed as cell growth inhibition incubated for 4 days by CellTiter-Glo asssay
|
[PMID: 34141084] |
SI-109 exerts a moderate growth inhibitory activity in MOLM-16 cells (IC50=3 μM)[1].
SI-109 is ineffective in inhibition of STAT3 Y705 phosphorylation and in suppression of c-Myc expression at concentrations as high as 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2429877-30-3
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Appearance Solid
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분자량 835.79
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화학식 C40H44F2N7O9P
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Color White to off-white
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SMILES
O=C([C@@H](NC([C@@H]1CC[C@H](CCN(C(C)=O)C[C@@H]2NC(C3=CC(C=C(C(F)(P(O)(O)=O)F)C=C4)=C4N3)=O)N1C2=O)=O)CCC(N)=O)NC(C5=CC=CC=C5)C6=CC=CC=C6
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선적
Shipping with dry ice.
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보관
-80°C, stored under nitrogen
Publications (2)
용액&용해도
DMSO : 100 mg/mL (119.65 mM; ultrasonic and warming and heat to 60°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 (stored under nitrogen). When stored at -80°C, please use it within 6 months.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months.
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: ≥ 2.5 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (2.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
순도&문서
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Data Sheet (277 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)
- 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1965 mL | 5.9824 mL | 11.9647 mL | 29.9118 mL |
| 5 mM | 0.2393 mL | 1.1965 mL | 2.3929 mL | 5.9824 mL | |
| 10 mM | 0.1196 mL | 0.5982 mL | 1.1965 mL | 2.9912 mL | |
| 15 mM | 0.0798 mL | 0.3988 mL | 0.7976 mL | 1.9941 mL | |
| 20 mM | 0.0598 mL | 0.2991 mL | 0.5982 mL | 1.4956 mL | |
| 25 mM | 0.0479 mL | 0.2393 mL | 0.4786 mL | 1.1965 mL | |
| 30 mM | 0.0399 mL | 0.1994 mL | 0.3988 mL | 0.9971 mL | |
| 40 mM | 0.0299 mL | 0.1496 mL | 0.2991 mL | 0.7478 mL | |
| 50 mM | 0.0239 mL | 0.1196 mL | 0.2393 mL | 0.5982 mL | |
| 60 mM | 0.0199 mL | 0.0997 mL | 0.1994 mL | 0.4985 mL | |
| 80 mM | 0.0150 mL | 0.0748 mL | 0.1496 mL | 0.3739 mL | |
| 100 mM | 0.0120 mL | 0.0598 mL | 0.1196 mL | 0.2991 mL |
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