M-808
Based on 1 Customer Validation
M-808 is a highly potent and efficacious covalent Menin-MLL interaction inhibitor, with a binding IC50 value of 2.6 nM.
For research use only. We do not sell to patients.
- Purity: 98.72%
- CAS No.: 2377335-74-3
- Formula: C45H63FN6O5S
- Molecular Weight:819.08
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
IC50: 1 nM (Menin-MLL in MV4;11 cells), 4 nM (Menin-MLL in MOLM-13 cells)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
2.8 μM
Compound: 16; M-808
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Growth inhibition of human HL60 cells after 7 days by WST-8 assay
Growth inhibition of human HL60 cells after 7 days by WST-8 assay
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[PMID: 32338903] |
| MOLM-13 | IC50 |
0.004 μM
Compound: 16; M-808
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Growth inhibition of human MOLM13 cells after 7 days by WST-8 assay
Growth inhibition of human MOLM13 cells after 7 days by WST-8 assay
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[PMID: 32338903] |
| MV4-11 | IC50 |
0.001 μM
Compound: 16; M-808
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Growth inhibition of human MV4-11 cells after 7 days by WST-8 assay
Growth inhibition of human MV4-11 cells after 7 days by WST-8 assay
|
[PMID: 32338903] |
M808 exhibits IC50 values of 1 nM, 4 nM and 2.8 nM in MV4;11 cells, MOLM-13 cells and HL60 cells, respectively[1].
M808 forms a covalent bond between its acrylamide and the sulfur atom of Cys329 in menin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2377335-74-3
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Appearance Solid
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Molecular Weight 819.08
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Formula C45H63FN6O5S
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Color White to off-white
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SMILES
O=S(C(C=C1)=CC=C1N(C2)CC2CN(CC3)CCC3[C@@]([C@@]4([H])CCC[C@@H]4NC(OC)=O)(CN5CCC5)C6=CC(F)=CC=C6)(C7CN(C(/C=C/CN8CCCCC8)=O)C7)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (122.09 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 (protect from light). 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). 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 (3.05 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 (3.05 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)
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 (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). 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 | 1.2209 mL | 6.1044 mL | 12.2088 mL | 30.5220 mL |
| 5 mM | 0.2442 mL | 1.2209 mL | 2.4418 mL | 6.1044 mL | |
| 10 mM | 0.1221 mL | 0.6104 mL | 1.2209 mL | 3.0522 mL | |
| 15 mM | 0.0814 mL | 0.4070 mL | 0.8139 mL | 2.0348 mL | |
| 20 mM | 0.0610 mL | 0.3052 mL | 0.6104 mL | 1.5261 mL | |
| 25 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 1.2209 mL | |
| 30 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0174 mL | |
| 40 mM | 0.0305 mL | 0.1526 mL | 0.3052 mL | 0.7631 mL | |
| 50 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6104 mL | |
| 60 mM | 0.0203 mL | 0.1017 mL | 0.2035 mL | 0.5087 mL | |
| 80 mM | 0.0153 mL | 0.0763 mL | 0.1526 mL | 0.3815 mL | |
| 100 mM | 0.0122 mL | 0.0610 mL | 0.1221 mL | 0.3052 mL |