MRT-3486
Based on 1 Customer Validation
MRT-3486 is a molecular glue degrader.MRT-3486 induces ternary complex formation between CRBN and predicted β-hairpin G-loop proteins.MRT-3486 is selected from an internal compound library for proximity-ligation experiments.
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- Pureté: 99.62%
- Formule: C29H28N6O5S
- Masse moléculaire:572.63
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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NEK7 |
Cereblon-DDB1 |
MRT-3486 (1-100 μM; 30 min-24 h) potently induces the formation of a dose-dependent ternary complex between CRBN and NEK7 in vitro, as well as in HEK293T and CAL51 cells[1].
MRT-3486 (80 μM; 1 h) drives the selective degradation of wild-type NEK7 in a reaction system containing 70 μM NEK7, 70 μM CRBN/DDB1, and 70 μM ADP, but does not degrade G-loop or N-terminal deletion mutants[1].
MRT-3486 can also form a structurally unique ternary complex with CRBN and NEK7, and the formation of this complex depends on the β-hairpin G-loop and the extended N-terminal interface[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Masse moléculaire 572.63
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Formule C29H28N6O5S
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Color White to off-white
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SMILES
O=C([C@H]1N(S(=O)(CC2=CC=CC=C2)=O)CC3=C(C=CC=C3)C1)NCC4=CC5=NC=C(N(C(N6)=O)CCC6=O)N5C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (174.63 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 (4.37 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 (4.37 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.
Pureté et documentation
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Fiche technique (275 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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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 1.7463 mL | 8.7316 mL | 17.4633 mL | 43.6582 mL |
| 5 mM | 0.3493 mL | 1.7463 mL | 3.4927 mL | 8.7316 mL | |
| 10 mM | 0.1746 mL | 0.8732 mL | 1.7463 mL | 4.3658 mL | |
| 15 mM | 0.1164 mL | 0.5821 mL | 1.1642 mL | 2.9105 mL | |
| 20 mM | 0.0873 mL | 0.4366 mL | 0.8732 mL | 2.1829 mL | |
| 25 mM | 0.0699 mL | 0.3493 mL | 0.6985 mL | 1.7463 mL | |
| 30 mM | 0.0582 mL | 0.2911 mL | 0.5821 mL | 1.4553 mL | |
| 40 mM | 0.0437 mL | 0.2183 mL | 0.4366 mL | 1.0915 mL | |
| 50 mM | 0.0349 mL | 0.1746 mL | 0.3493 mL | 0.8732 mL | |
| 60 mM | 0.0291 mL | 0.1455 mL | 0.2911 mL | 0.7276 mL | |
| 80 mM | 0.0218 mL | 0.1091 mL | 0.2183 mL | 0.5457 mL | |
| 100 mM | 0.0175 mL | 0.0873 mL | 0.1746 mL | 0.4366 mL |
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