MI-136
Based on 1 publication(s) in Google Scholar
MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.
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- Pureza: 99.04%
- No. CAS: 1628316-74-4
- Fòrmula: C23H21F3N6S
- Peso molecular:470.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) MI-136
More
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Bone marrow cell | GI50 |
0.55 μM
Compound: 1; MI-136
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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 |
3 μM
Compound: 1; MI-136
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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-136 (0-20) exhibits IC50values of 5.59 μM, 7.15 μM, 5.37 μM and 19.76 μM in LNCaP, VCaP, 22rv1 and PNT2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AR positive cell lines such as VCaP, LNCaP and 22RV1.
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Concentration:0-20 μM.
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Incubation Time:24 h.
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Result:Inhibited cell proliferation.
MI-136 (40 mg/kg, ip) leads to a significant decrease in the growth of castration-resistant VCaP tumors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:VCaP xenografts[2].
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Dosage:40 mg/kg.
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Administration:Intraperitoneal injection, 5 days a week.
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Result:Led to a significant decrease in the growth of castration-resistant VCaP tumors compared to vehicle controls.
Chemical Information
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No. CAS 1628316-74-4
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Appearance Solid
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Peso molecular 470.51
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Fòrmula C23H21F3N6S
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Color White to off-white
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SMILES
FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(NC(C#N)=C5)C5=C4)CC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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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
Solvente y solubilidad
DMSO : 110 mg/mL (233.79 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: ≥ 2.75 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
Pureza y Documentación
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Ficha de datos (275 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Dmitry Borkin, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913. [Content Brief]
[2]. Rohit Malik, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015 Apr;21(4):344-52. [Content Brief]
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 | 2.1254 mL | 10.6268 mL | 21.2535 mL | 53.1338 mL |
| 5 mM | 0.4251 mL | 2.1254 mL | 4.2507 mL | 10.6268 mL | |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1254 mL | 5.3134 mL | |
| 15 mM | 0.1417 mL | 0.7085 mL | 1.4169 mL | 3.5423 mL | |
| 20 mM | 0.1063 mL | 0.5313 mL | 1.0627 mL | 2.6567 mL | |
| 25 mM | 0.0850 mL | 0.4251 mL | 0.8501 mL | 2.1254 mL | |
| 30 mM | 0.0708 mL | 0.3542 mL | 0.7085 mL | 1.7711 mL | |
| 40 mM | 0.0531 mL | 0.2657 mL | 0.5313 mL | 1.3283 mL | |
| 50 mM | 0.0425 mL | 0.2125 mL | 0.4251 mL | 1.0627 mL | |
| 60 mM | 0.0354 mL | 0.1771 mL | 0.3542 mL | 0.8856 mL | |
| 80 mM | 0.0266 mL | 0.1328 mL | 0.2657 mL | 0.6642 mL | |
| 100 mM | 0.0213 mL | 0.1063 mL | 0.2125 mL | 0.5313 mL |
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