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| 25mg |
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Purity: ≥98%
MI-3 (Menin-MLL Inhibitor 3) is a novel and potent inhibitor of menin-MLL interaction with potential antitumor activity. It inhibits menin-MLL interaction with an IC50 of 648 nM. It exhibits excellent antiproliferative activity against various cancer cells.
| ln Vitro |
In human cells, treatment with MI-3 (12.5-50 μM; HEK293 cells) efficiently suppresses the menin-MLL-AF9 interaction[1]. In KOPN-8, MV4, and ME-1 cells, MI-3 (0-1.6 μM; 72 hours; 11 cells) treatment demonstrates an efficient and dose-dependent growth inhibition[1]. The administration of MI-3 (12.5-50 μM; 48 hours; MV4; 11 cells) causes a significant, dose-dependent rise in the number of Annexin V and Annexin V/propidium iodide (PI) cells, indicating an increase in apoptosis[1]. The treatment of THP-1 cells with MI-3 (6.25-25 μM; 6 days) significantly lowers the expression of MEIS1 and HOXA9.
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| ln Vivo |
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293 cells Tested Concentrations: 12.5 μM, 25 μM, 50 μM Incubation Duration: Experimental Results: Very effectively inhibited the menin-MLL-AF9 interaction in human cells. Cell Viability Assay[1] Cell Types: KOPN-8 and MV4;11 cells Tested Concentrations: 0 μM, 0.4 μM, 0.8 μM, 1.2 μM, 1.6 μM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated an effective and dose-dependent growth inhibition in KOPN-8 and MV4;11 cells. |
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| References |
[1]. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology (2012), 8(3), 277-284.
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| Molecular Formula |
C18H25N5S2
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| Molecular Weight |
375.55
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| CAS # |
1271738-59-0
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| Related CAS # |
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| SMILES |
CC(C)C1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1
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| InChi Key |
FUGQNAUKABUDQI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H25N5S2/c1-12(2)14-9-13-15(20-11-21-16(13)24-14)22-5-7-23(8-6-22)17-19-10-18(3,4)25-17/h9,11-12H,5-8,10H2,1-4H3
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| Chemical Name |
4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-propan-2-ylthieno[2,3-d]pyrimidine
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6628 mL | 13.3138 mL | 26.6276 mL | |
| 5 mM | 0.5326 mL | 2.6628 mL | 5.3255 mL | |
| 10 mM | 0.2663 mL | 1.3314 mL | 2.6628 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02566954 | Completed | Other: 3D measurement of the lower limb by EOS |
Limb Deformities | Fondation Lenval | May 25, 2014 | Not Applicable |
| NCT05168033 | Recruiting | Other: Motor imagery training Other: Classic rehabilitation |
Anterior Cruciate Ligament Rupture Motor Imagery |
University Ghent | November 15, 2021 | Not Applicable |
| NCT05118451 | Recruiting | Procedure: 3 d visualization technology | Primary Liver Cancers | Zhujiang Hospital | July 1, 2020 | Not Applicable |
| NCT01132430 | Completed | Behavioral: Motivational interviewing Behavioral: Usual care |
Asthma | Hopital du Sacre-Coeur de Montreal | June 2008 | Phase 3 |
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