MRT-23227
Based on 1 Customer Validation
MRT-23227 is a CRBN-recruiting molecular glue degrader targeting VAV1. MRT-23227 binds to the tryptophan triad pocket of CRBN, forms a ternary complex with the SH3c domain of VAV1, and induces proteasomal degradation of VAV1 through hydrogen-bond interactions between CRBN residues and the RT loop and side chains of VAV1. MRT-23227 can be used in the research of T-cell leukemia and lymphoma.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 3050683-03-6
- Formula: C22H20ClN3O3
- Molecular Weight:409.87
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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
MRT-23227 acts as a CRBN-recruiting molecular glue degrader that induces VAV1 degradation via surface mimicry of GSPT1 by VAV1's SH3c domain, expanding the targetable neosubstrate space beyond canonical β-hairpin G-loop proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3050683-03-6
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Appearance Solid
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Molecular Weight 409.87
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Formula C22H20ClN3O3
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Color White to off-white
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SMILES
O=C(C(C1=C(Cl)C(C2=CC=C(OCC3=NN(C)C=C3)C=C2)=CC=C1)CC4)NC4=O
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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 : 100 mg/mL (243.98 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 (6.10 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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 (6.10 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.
Purity & Documentation
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Data Sheet (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 2.4398 mL | 12.1990 mL | 24.3980 mL | 60.9950 mL |
| 5 mM | 0.4880 mL | 2.4398 mL | 4.8796 mL | 12.1990 mL | |
| 10 mM | 0.2440 mL | 1.2199 mL | 2.4398 mL | 6.0995 mL | |
| 15 mM | 0.1627 mL | 0.8133 mL | 1.6265 mL | 4.0663 mL | |
| 20 mM | 0.1220 mL | 0.6099 mL | 1.2199 mL | 3.0497 mL | |
| 25 mM | 0.0976 mL | 0.4880 mL | 0.9759 mL | 2.4398 mL | |
| 30 mM | 0.0813 mL | 0.4066 mL | 0.8133 mL | 2.0332 mL | |
| 40 mM | 0.0610 mL | 0.3050 mL | 0.6099 mL | 1.5249 mL | |
| 50 mM | 0.0488 mL | 0.2440 mL | 0.4880 mL | 1.2199 mL | |
| 60 mM | 0.0407 mL | 0.2033 mL | 0.4066 mL | 1.0166 mL | |
| 80 mM | 0.0305 mL | 0.1525 mL | 0.3050 mL | 0.7624 mL | |
| 100 mM | 0.0244 mL | 0.1220 mL | 0.2440 mL | 0.6099 mL |