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MI-3454

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Catalog No. T39584Cas No. 2134169-43-8

MI-3454 is an orally active, selective and potent inhibitor of Menin-MLL1 interaction that inhibits the proliferation and induces differentiation of acute leukemia cells with MLL1 translocation or NPM1 mutation.MI-3454 induces complete remission or regression of leukemia in a mouse model of leukemia with MLL1 rearrangement or NPM1 mutation through the down-regulation of key genes involved in leukemogenesis. complete remission or remission.

MI-3454

MI-3454

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Purity: 99.68%
Catalog No. T39584Cas No. 2134169-43-8
MI-3454 is an orally active, selective and potent inhibitor of Menin-MLL1 interaction that inhibits the proliferation and induces differentiation of acute leukemia cells with MLL1 translocation or NPM1 mutation.MI-3454 induces complete remission or regression of leukemia in a mouse model of leukemia with MLL1 rearrangement or NPM1 mutation through the down-regulation of key genes involved in leukemogenesis. complete remission or remission.
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1 mg$198-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.68%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
MI-3454 is an orally active, selective and potent inhibitor of Menin-MLL1 interaction that inhibits the proliferation and induces differentiation of acute leukemia cells with MLL1 translocation or NPM1 mutation.MI-3454 induces complete remission or regression of leukemia in a mouse model of leukemia with MLL1 rearrangement or NPM1 mutation through the down-regulation of key genes involved in leukemogenesis. complete remission or remission.
Targets&IC50
Menin-MLL1:0.51 nM
In vitro
In murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1, MI-3454 (0.001, 0.01, 0.1, 1, 10 μM; 7 days) demonstrated a significant reduction in cell proliferation[1].
In vivo
In 8- to 10-week-old female NSG mice (MV-4-11 xenotransplantation model of MLL leukemia), MI-3454 (120 mg/kg; orally; once or twice daily for 7 consecutive days) is sufficient to block leukemia progression[1].
Chemical Properties
Molecular Weight636.73
FormulaC32H35F3N8OS
Cas No.2134169-43-8
SmilesCNc1nc(NC2CCN(Cc3ccc4n(CC56CC(C5)(C6)NC=O)c(cc4c3C)C#N)CC2)c2cc(CC(F)(F)F)sc2n1
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 20 mg/mL (31.41 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5705 mL7.8526 mL15.7052 mL78.5262 mL
5 mM0.3141 mL1.5705 mL3.1410 mL15.7052 mL
10 mM0.1571 mL0.7853 mL1.5705 mL7.8526 mL
20 mM0.0785 mL0.3926 mL0.7853 mL3.9263 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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