TGF-βRI inhibitor 3
Based on 1 Customer Validation
TGF-βRI inhibitor 3 (Compound 9ac) is a selective TGF-β inhibitor. TGF-βRI inhibitor 3 can effectively inhibit the TGF-β signaling pathway. TGF-βRI inhibitor 3 has IC50 values of 13 μM and 0.63 μM for c-Src kinase and ALK5 kinase, respectively.
For research use only. We do not sell to patients.
- Purity: 99.16%
- CAS No.: 666729-57-3
- Formula: C21H21NO4
- Molecular Weight:351.40
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.37 μM
Compound: 9ac
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Inhibition of TGF-beta expressed in human A549 cells assessed as luciferase activity after 4 hrs by Smad2/3 reporter assay
Inhibition of TGF-beta expressed in human A549 cells assessed as luciferase activity after 4 hrs by Smad2/3 reporter assay
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[PMID: 18479116] |
| A549 | IC50 |
0.5 μM
Compound: 9ac
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Inhibition of TGF-beta mediated Smad2 phosphorylation in human A549 cells after 30 mins by Western blot
Inhibition of TGF-beta mediated Smad2 phosphorylation in human A549 cells after 30 mins by Western blot
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[PMID: 18479116] |
Chemical Information
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CAS No. 666729-57-3
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Appearance Solid
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Molecular Weight 351.40
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Formula C21H21NO4
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Color Light yellow to yellow
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SMILES
CC(C1=CC(C)=C(C)C=C1OC2=CC=NC3=CC(OC)=C(OC)C=C23)=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 : 100 mg/mL (284.58 mM; Need ultrasonic; 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 (7.11 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.
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 (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 2.8458 mL | 14.2288 mL | 28.4576 mL | 71.1440 mL |
| 5 mM | 0.5692 mL | 2.8458 mL | 5.6915 mL | 14.2288 mL | |
| 10 mM | 0.2846 mL | 1.4229 mL | 2.8458 mL | 7.1144 mL | |
| 15 mM | 0.1897 mL | 0.9486 mL | 1.8972 mL | 4.7429 mL | |
| 20 mM | 0.1423 mL | 0.7114 mL | 1.4229 mL | 3.5572 mL | |
| 25 mM | 0.1138 mL | 0.5692 mL | 1.1383 mL | 2.8458 mL | |
| 30 mM | 0.0949 mL | 0.4743 mL | 0.9486 mL | 2.3715 mL | |
| 40 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7786 mL | |
| 50 mM | 0.0569 mL | 0.2846 mL | 0.5692 mL | 1.4229 mL | |
| 60 mM | 0.0474 mL | 0.2371 mL | 0.4743 mL | 1.1857 mL | |
| 80 mM | 0.0356 mL | 0.1779 mL | 0.3557 mL | 0.8893 mL | |
| 100 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.7114 mL |
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