| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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MM-102 TFA (the trifluoroacetic acid salt of MM-102) is a novel, potent, high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay. MM-102 reduces the expression of MLL1 targeted genes HoxA9 and Meis-1 in MLL1-AF9 transduced murine cells. Since these two genes are required for MLL1 mediated leukemogenesis, MM-102 is found to inhibit cell growth of leukemia cells harboring MLL1 fusion proteins. It dose-dependently inhibits the cell growth in the MV4;11 and KOPN8 cell lines with IC50 values both of 25μM.
| ln Vitro |
In leukemia cells carrying the MLL1-AF9 fusion gene, MM-102 (HMTase Inhibitor IX) reduces MLL1 methyltransferase activity as well as MLL-1-induced HoxA9 and Meis-1 gene expression. Leukemia cells containing MLL1 fusion proteins also experienced reduced cell proliferation and death. With an IC50 of 0.4-0.9 μM in the HMT experiment, MM-102 (TFA) exhibits the most inhibitory action and the highest binding affinity for WDR5[1]. Leukemia cell lines carrying the MLL1-AF4 and MLL1-ENL fusion proteins, MV4;11 and KOPN8, respectively, are inhibited in their ability to proliferate by MM-102 (HMTase inhibitor IX) in a dose-dependent manner [1]. MM-102, also known as HMTase Inhibitor IX, totally suppresses cell growth in these cell lines at 75 μM, with an IC50 of 25 μM[1]. Leukemia cells are effectively and selectively inhibited in their proliferation and induced to undergo apoptosis by MM-102 (HMTase inhibitor IX). Leukemia cells are not significantly affected by MLL1 fusion protein or wild-type MLL1 protein [1].
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| ln Vivo |
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| Animal Protocol |
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| References |
[1]. Karatas H, et al. High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interaction. J Am Chem Soc. 2013 Jan 16;135(2):669-682
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| Molecular Formula |
C37H50F5N7O6
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|---|---|
| Molecular Weight |
783.828226566315
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| CAS # |
1883545-52-5
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| Related CAS # |
MM-102;1417329-24-8
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| SMILES |
FC1C=CC(=CC=1)C(C1C=CC(=CC=1)F)NC(C1(CCCC1)NC([C@H](CCC/N=C(\N)/N)NC(C(CC)(CC)NC(C(C)C)=O)=O)=O)=O.FC(C(=O)O)(F)F
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ≥ 100 mg/mL (~127.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.19 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (3.19 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 25.0 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: ≥ 2.5 mg/mL (3.19 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 | 1.2758 mL | 6.3789 mL | 12.7579 mL | |
| 5 mM | 0.2552 mL | 1.2758 mL | 2.5516 mL | |
| 10 mM | 0.1276 mL | 0.6379 mL | 1.2758 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.
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