C188
Based on 1 Customer Validation
C188 (CPD188) is a STAT3 inhibitor with anticancer effects. C188 inhibits STAT3 SH2/pY-peptide binding (IC50 of 20 µM against pY-peptide binding) and IL-6-mediated STAT3 phosphorylation. C188 is selective for STAT3 over STAT1. C188 inhibits nuclear-to-cytoplasmic translocation of Stat3. C188 shows highly active induces apoptosis in breast cancer cell lines with constitutive Stat3 activation (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively).
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- Purity: 98.29%
- CAS No.: 823828-18-8
- 화학식: C19H15NO7S2
- 분자량:433.45
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
21 μM
Compound: 20
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Growth inhibition of human DU145 cells after 2 days by MTT assay
Growth inhibition of human DU145 cells after 2 days by MTT assay
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[PMID: 22309208] |
| HepG2 | IC50 |
73 μM
Compound: 39
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Inhibition of IL6-mediated STAT3 phosphorylation in human HepG2 cells preincubated for 1 hr prior to IL6 challenge measured after 30 mins by immunoblot analysis
Inhibition of IL6-mediated STAT3 phosphorylation in human HepG2 cells preincubated for 1 hr prior to IL6 challenge measured after 30 mins by immunoblot analysis
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[PMID: 22650325] |
| HT-29 | GI50 |
4.4 μM
Compound: 20
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Growth inhibition of human HT-29 cells after 2 days by MTT assay
Growth inhibition of human HT-29 cells after 2 days by MTT assay
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[PMID: 22309208] |
| MDA-MB-468 | EC50 |
0.73 μM
Compound: 53; C188
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Induction of apoptosis in human MDA-MB-468 cells incubated for 24 hrs by ELISA assay
Induction of apoptosis in human MDA-MB-468 cells incubated for 24 hrs by ELISA assay
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[PMID: 31810784] |
C188 (CPD188) (0-300 μM; 24 h) shows preferentially induces apoptosis in cultures expressing constitutively active STAT3 (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively), while being less effective against cells without constitutively active STAT3 (EC50s of 15.5 µM and 17.19 µM in MDA-MB-453 and MCF7 cultures, respectively)[1].
C188 (1-300 µM; pretreated for 60 min, then stimulated with IL-6 (30 ng/mL) for 30 min) inhibits IL-6-mediated tyrosine phosphorylation of Stat3 in the immunoblot assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468, MDA-MB-231, MDA-MB-435, MDA-MB-453, MCF7 cells
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Concentration:0, 0.1, 0.3, 1, 3, 10, 30, 100, 300 μM
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Incubation Time:24 hours
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Result:Induced apoptosis of MDA-MB-468, MDA-MB-231 and MDA-MB-435 cell lines with constitutive Stat3 activity in a dose-dependent manner.
Had detectable activity against MDA-MB-453 and MCF7 cell lines, but showed preferential activity against cell lines with constitutive Stat3 activity.
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Cell Line:HepG2 cells
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Concentration:1, 3, 10, 30, 100, 300 µM
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Incubation Time:Pretreated for 60 min; then stimulated with IL-6 (30 ng/mL) for 30 min
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Result:
Chemical Information
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CAS No. 823828-18-8
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Appearance Solid
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분자량 433.45
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화학식 C19H15NO7S2
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Color Off-white to light yellow
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SMILES
O=C(O)C1=CC=C(S(=O)(NC2=C3C=CC=CC3=C(O)C(SCC(O)=O)=C2)=O)C=C1
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Synonyms
CPD188
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (230.71 mM; Need ultrasonic and warming; 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: ≥ 2.5 mg/mL (5.77 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 (5.77 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 (279 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 | 2.3071 mL | 11.5354 mL | 23.0707 mL | 57.6768 mL |
| 5 mM | 0.4614 mL | 2.3071 mL | 4.6141 mL | 11.5354 mL | |
| 10 mM | 0.2307 mL | 1.1535 mL | 2.3071 mL | 5.7677 mL | |
| 15 mM | 0.1538 mL | 0.7690 mL | 1.5380 mL | 3.8451 mL | |
| 20 mM | 0.1154 mL | 0.5768 mL | 1.1535 mL | 2.8838 mL | |
| 25 mM | 0.0923 mL | 0.4614 mL | 0.9228 mL | 2.3071 mL | |
| 30 mM | 0.0769 mL | 0.3845 mL | 0.7690 mL | 1.9226 mL | |
| 40 mM | 0.0577 mL | 0.2884 mL | 0.5768 mL | 1.4419 mL | |
| 50 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL | 1.1535 mL | |
| 60 mM | 0.0385 mL | 0.1923 mL | 0.3845 mL | 0.9613 mL | |
| 80 mM | 0.0288 mL | 0.1442 mL | 0.2884 mL | 0.7210 mL | |
| 100 mM | 0.0231 mL | 0.1154 mL | 0.2307 mL | 0.5768 mL |
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