MS15 TFA
Based on 1 Customer Validation
MS15 TFA is a potent and selective AKT PROTAC degrader. MS15 TFA inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively.
(Pink: Akt ligand (HY-19719); Blue: VHL ligand (HY-112078); Black: linker (HY-128421)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.82%
- Fòrmula: C66H80F3N11O7S
- Peso molecular:1228.47
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Almacenamiento:
-80°C, protect from light, stored under nitrogen
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
MS15 TFA (0-10 μM, 24 h) potently induces AKT degradation in SW620 cells and MS21-resistant KRAS/BRAF mutant cells[1].
MS15 TFA (0-10 μM, 5 days) inhibits the proliferation of KRAS mutant SW620 cells[1].
MS15 TFA (1 μM, 1-24 h) mediates AKT degradation in a time- and UPS-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620 cells, Colo205, HT-29, SKMEL 239, and PANC-1 cells
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Concentration:1 nM, 3 nM, 10 nM, 30 nM, 100 nM, 300 nM, 1 μM, 3 μM, 10 μM
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Incubation Time:24 h
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Result:Effectively induced T-AKT degradation in a concentration-dependent manner, with a DC50 value of 23 ± 16 nM in SW620 cells. Nearly complete AKT degradation was achieved at a concentration of 100 nM in SW620 cells and PANC-1 cells. Induced AKT degradation at 1 μM in BRAF mutant cell lines, such as Colo205, HT-29, and SKMEL 239 cells.
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Cell Line:SW620 cells
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Concentration:0 nM, 30 nM, 100 nM, 1 μM, 3 μM, 10 μM
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Incubation Time:5 days
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Result:Displayed slightly better antiproliferative activity than Miransertib (HY-19719), with a GI50 of 3.1 ± 0.3 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Swiss albino mice[1]
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Dosage:75 mg/kg
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Administration:IP, once (Pharmacokinetic Analysis)
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Result:The maximum plasma concentration (Cmax = 1 μM) was achieved at 0.5 h post-treatment, and plasma concentrations were maintained above 100 nM for at least 12 h.Could achieve enough plasma exposure for effective AKT degradation.
Chemical Information
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Appearance Solid
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Peso molecular 1228.47
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Fòrmula C66H80F3N11O7S
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Color White to yellow
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SMILES
NC1(CCC1)C(C=C2)=CC=C2N3C4=NC(C5=CC(CCC(NCCCCCCCCCCC(N[C@H](C(N6C[C@@H](C[C@H]6C(N[C@@H](C)C7=CC=C(C=C7)C8=C(N=CS8)C)=O)O)=O)C(C)(C)C)=O)=O)=CC=C5)=CC=C4N=C3C9=CC=CN=C9N.OC(C(F)(F)F)=O
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Envío
Shipping with dry ice.
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Almacenamiento
-80°C, protect from light, stored under nitrogen
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (81.40 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months.
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months.
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 (2.04 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.
Pureza y Documentación
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Ficha de datos (282 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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Instrucciones de manejo (2659 KB)
Referencias
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.8140 mL | 4.0701 mL | 8.1402 mL | 20.3505 mL |
| 5 mM | 0.1628 mL | 0.8140 mL | 1.6280 mL | 4.0701 mL | |
| 10 mM | 0.0814 mL | 0.4070 mL | 0.8140 mL | 2.0351 mL | |
| 15 mM | 0.0543 mL | 0.2713 mL | 0.5427 mL | 1.3567 mL | |
| 20 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0175 mL | |
| 25 mM | 0.0326 mL | 0.1628 mL | 0.3256 mL | 0.8140 mL | |
| 30 mM | 0.0271 mL | 0.1357 mL | 0.2713 mL | 0.6784 mL | |
| 40 mM | 0.0204 mL | 0.1018 mL | 0.2035 mL | 0.5088 mL | |
| 50 mM | 0.0163 mL | 0.0814 mL | 0.1628 mL | 0.4070 mL | |
| 60 mM | 0.0136 mL | 0.0678 mL | 0.1357 mL | 0.3392 mL | |
| 80 mM | 0.0102 mL | 0.0509 mL | 0.1018 mL | 0.2544 mL |
MS15 TFA Related Classifications
HY-151613A Related Classifications
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