ATH686
Based on 1 Customer Validation
ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects.
For research use only. We do not sell to patients.
- Purity: 99.54%
- CAS No.: 853299-52-2
- Formula: C25H28F3N7O2
- Molecular Weight:515.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
ATH686 (1-100 µM; 3 days) potently inhibits cell proliferation (IC50 around 0.001 µM) via induction of apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells[1].
ATH686 (10 nM; for 15 minutes) inhibits autophosphorylation of mutant FLT3 in FLT3-ITD-Ba/F3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells
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Concentration:1, 5, 10, 50, 100 µM
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Incubation Time:3 days
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Result:Potently inhibited cell proliferation (IC50 around 0.001 µM) via induction of apoptosis.
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Cell Line:FLT3-ITD-Ba/F3 cells
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Concentration:10 nM
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Incubation Time:For 15 minutes
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Result:Inhibited autophosphorylation of mutant FLT3, with no apparent reduction in levels of the FLT3 protein.
Chemical Information
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CAS No. 853299-52-2
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Appearance Solid
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Molecular Weight 515.53
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Formula C25H28F3N7O2
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Color Light yellow to light brown
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SMILES
NC1=NC(OC2=CC=C(NC(NC3=CC(C(F)(F)F)=C(CN4CCN(CC)CC4)C=C3)=O)C=C2)=CC=N1
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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 : 250 mg/mL (484.94 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: ≥ 2.08 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (273 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 | 1.9398 mL | 9.6988 mL | 19.3975 mL | 48.4938 mL |
| 5 mM | 0.3880 mL | 1.9398 mL | 3.8795 mL | 9.6988 mL | |
| 10 mM | 0.1940 mL | 0.9699 mL | 1.9398 mL | 4.8494 mL | |
| 15 mM | 0.1293 mL | 0.6466 mL | 1.2932 mL | 3.2329 mL | |
| 20 mM | 0.0970 mL | 0.4849 mL | 0.9699 mL | 2.4247 mL | |
| 25 mM | 0.0776 mL | 0.3880 mL | 0.7759 mL | 1.9398 mL | |
| 30 mM | 0.0647 mL | 0.3233 mL | 0.6466 mL | 1.6165 mL | |
| 40 mM | 0.0485 mL | 0.2425 mL | 0.4849 mL | 1.2123 mL | |
| 50 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9699 mL | |
| 60 mM | 0.0323 mL | 0.1616 mL | 0.3233 mL | 0.8082 mL | |
| 80 mM | 0.0242 mL | 0.1212 mL | 0.2425 mL | 0.6062 mL | |
| 100 mM | 0.0194 mL | 0.0970 mL | 0.1940 mL | 0.4849 mL |