MI-463
Based on 2 publication(s) in Google Scholar
MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 1628317-18-9
- Formula: C24H23F3N6S
- Molecular Weight:484.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MI-463
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| Bone marrow cell | GI50 |
0.2 μM
Compound: 14; MI-463
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Growth inhibition of MLL-AF9 transformed mouse bone marrow cells after 7 days by MTT assay
Growth inhibition of MLL-AF9 transformed mouse bone marrow cells after 7 days by MTT assay
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[PMID: 26744767] |
| Bone marrow cell | GI50 |
5.6 μM
Compound: 14; MI-463
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Growth inhibition of Hoxa9/Meis1 transformed mouse bone marrow cells after 7 days by MTT assay
Growth inhibition of Hoxa9/Meis1 transformed mouse bone marrow cells after 7 days by MTT assay
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[PMID: 26744767] |
MI-463 can reach the target protein in mammalian cells and effectively inhibit the menin-mLL-AF9 interaction at sub-micromolar concentrations. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-463 results in substantial growth inhibition, with GI50 of 0.23 μM[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. 1628317-18-9
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Appearance Solid
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Molecular Weight 484.54
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Formula C24H23F3N6S
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Color White to light yellow
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SMILES
FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(NC(C#N)=C5)C5=C4C)CC3
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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 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
A histone-centric multi-omics study shows that increased H3K4 methylation sustains triple-negative breast cancer phenotypes. [Abstract]2025 Sep 30;16(1):8716. PMID: 41028718 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273
Solvent & Solubility
DMSO : 100 mg/mL (206.38 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (4.29 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (4.29 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol
Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed at day 4, viable cell numbers are restored to the original concentration and MI-463 are re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×106 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or compounds (MI-463 or MI-503) are administrated once daily at designated doses using i.p. injections[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0638 mL | 10.3191 mL | 20.6381 mL | 51.5953 mL |
| 5 mM | 0.4128 mL | 2.0638 mL | 4.1276 mL | 10.3191 mL | |
| 10 mM | 0.2064 mL | 1.0319 mL | 2.0638 mL | 5.1595 mL | |
| 15 mM | 0.1376 mL | 0.6879 mL | 1.3759 mL | 3.4397 mL | |
| 20 mM | 0.1032 mL | 0.5160 mL | 1.0319 mL | 2.5798 mL | |
| 25 mM | 0.0826 mL | 0.4128 mL | 0.8255 mL | 2.0638 mL | |
| 30 mM | 0.0688 mL | 0.3440 mL | 0.6879 mL | 1.7198 mL | |
| 40 mM | 0.0516 mL | 0.2580 mL | 0.5160 mL | 1.2899 mL | |
| 50 mM | 0.0413 mL | 0.2064 mL | 0.4128 mL | 1.0319 mL | |
| 60 mM | 0.0344 mL | 0.1720 mL | 0.3440 mL | 0.8599 mL | |
| 80 mM | 0.0258 mL | 0.1290 mL | 0.2580 mL | 0.6449 mL | |
| 100 mM | 0.0206 mL | 0.1032 mL | 0.2064 mL | 0.5160 mL |
MI-463 Related Classifications
HY-19809 Related Classifications
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