AK-068
Based on 1 Customer Validation
AK-068 is a high-affinity and selective STAT6 ligand, with a Ki of 6 nM. AK-068 demonstrates at least >150- and >85-fold binding selectivity over STAT5A (Ki >1 μM) and STAT5B (Ki >500 μM) proteins, respectively. AK-068 is a ligand for target protein for PROTAC, can be used for synthesis of PROTACs.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 2982851-09-0
- Formula: C31H36F2N3O7PS
- Molecular Weight:663.67
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Biological Activity
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STAT6 6 nM (Ki) |
STAT5a >1 μM (Ki) |
STAT5b >500 μM (Ki) |
AK-068 can be used for synthesis of PROTAC AK-1690 (HY-169179)[1].
AK-068 (10 μM, 12-24 h) fails to inhibit phosphorylation of STAT6 protein in MV4;11, PBMCs and L1236 cells alone[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4;11, PBMCs and L1236 cells
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Concentration:10 μM
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Incubation Time:12 h for MV4;11, 18 h for PBMCs, 24 h for L1236 cells
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Result:Had no effect on the levels of STAT6 and STAT6Y641 protein.
Chemical Information
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CAS No. 2982851-09-0
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Appearance Solid
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Molecular Weight 663.67
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Formula C31H36F2N3O7PS
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Color White to off-white
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SMILES
FC(C1=CC=C2C(C=C(C(N[C@@H](C(C)(C)C)C(N3[C@H](C(N4C[C@@H](C5=CC=CC=C5)OCC4)=O)CCC3)=O)=O)S2)=C1)(P(O)(O)=O)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : ≥ 100 mg/mL (150.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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 (3.77 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 (3.77 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light, stored under nitrogen). 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 | 1.5068 mL | 7.5339 mL | 15.0677 mL | 37.6693 mL |
| 5 mM | 0.3014 mL | 1.5068 mL | 3.0135 mL | 7.5339 mL | |
| 10 mM | 0.1507 mL | 0.7534 mL | 1.5068 mL | 3.7669 mL | |
| 15 mM | 0.1005 mL | 0.5023 mL | 1.0045 mL | 2.5113 mL | |
| 20 mM | 0.0753 mL | 0.3767 mL | 0.7534 mL | 1.8835 mL | |
| 25 mM | 0.0603 mL | 0.3014 mL | 0.6027 mL | 1.5068 mL | |
| 30 mM | 0.0502 mL | 0.2511 mL | 0.5023 mL | 1.2556 mL | |
| 40 mM | 0.0377 mL | 0.1883 mL | 0.3767 mL | 0.9417 mL | |
| 50 mM | 0.0301 mL | 0.1507 mL | 0.3014 mL | 0.7534 mL | |
| 60 mM | 0.0251 mL | 0.1256 mL | 0.2511 mL | 0.6278 mL | |
| 80 mM | 0.0188 mL | 0.0942 mL | 0.1883 mL | 0.4709 mL | |
| 100 mM | 0.0151 mL | 0.0753 mL | 0.1507 mL | 0.3767 mL |