A 77-01
Based on 2 publication(s) in Google Scholar
A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
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- Reinheit: 99.92%
- CAS. Nr.: 607737-87-1
- Formel: C18H14N4
- Molecular Weight:286.33
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) A 77-01
More
Biologische Aktivität
IC50: 25 nM (ALK5)[1]
A-77-01 (0.01-10 μM; 25 hours; Mv1Lu cells) treatment effectively inhibits TGF-β-induced transcriptional activation in concentration-dependent fashion[1].
A-77-01 (1 μM; 24-72 hours; Mv1Lu cells) treatment efficiently prevents the growth-inhibitory effects of TGF-β[1].
A-77-01 (1 μM; 30 minutes; HaCaT cells) treatment inhibits TGF-β-induced phosphorylation of Smad2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mv1Lu cells
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Concentration:0.01 µM, 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, 10 µM
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Incubation Time:25 hours
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Result:Inhibited the luciferase activity induced by TGF-β in concentration-dependent fashion.
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Cell Line:Mv1Lu cells
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Concentration:1 µM
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Incubation Time:24 hours, 48 hours, 72 hours
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Result:Efficiently prevented the growth-inhibitory effects of TGF-β.
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Cell Line:HaCaT cells
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Concentration:1 µM
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Incubation Time:30 minutes
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Result:Inhibited TGF-β-induced phosphorylation of Smad2.
Chemical Information
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CAS. Nr. 607737-87-1
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Appearance Solid
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Molecular Weight 286.33
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Formel C18H14N4
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Color Off-white to light yellow
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SMILES
CC1=CC=CC(C2=NNC=C2C3=CC=NC4=CC=CC=C34)=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Mol Med Rep
MicroRNA-214-5p/TGF-β/Smad2 signaling alters adipogenic differentiation of bone marrow stem cells in postmenopausal osteoporosis. [Abstract]2018 May;17(5):6301-6310. PMID: 29532880 -
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (87.31 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (8.73 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 (8.73 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.
Reinheit & Dokumentation
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Data Sheet (280 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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4925 mL | 17.4624 mL | 34.9247 mL | 87.3118 mL |
| 5 mM | 0.6985 mL | 3.4925 mL | 6.9849 mL | 17.4624 mL | |
| 10 mM | 0.3492 mL | 1.7462 mL | 3.4925 mL | 8.7312 mL | |
| 15 mM | 0.2328 mL | 1.1642 mL | 2.3283 mL | 5.8208 mL | |
| 20 mM | 0.1746 mL | 0.8731 mL | 1.7462 mL | 4.3656 mL | |
| 25 mM | 0.1397 mL | 0.6985 mL | 1.3970 mL | 3.4925 mL | |
| 30 mM | 0.1164 mL | 0.5821 mL | 1.1642 mL | 2.9104 mL | |
| 40 mM | 0.0873 mL | 0.4366 mL | 0.8731 mL | 2.1828 mL | |
| 50 mM | 0.0698 mL | 0.3492 mL | 0.6985 mL | 1.7462 mL | |
| 60 mM | 0.0582 mL | 0.2910 mL | 0.5821 mL | 1.4552 mL | |
| 80 mM | 0.0437 mL | 0.2183 mL | 0.4366 mL | 1.0914 mL |
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