MI-463

Catalog No.S7816

MI-463 Chemical Structure

Molecular Weight(MW): 484.54

MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.

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Biological Activity

Description MI-463 is a potent inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.
Targets
Menin-MLL interaction [1]
(Cell-free assay)
15.3 nM
In vitro

MI-463 demonstrates profound on-target activity in MLL leukemia cells. MI-463 results in substantial growth inhibition, with half-maximal growth inhibitory concentration (GI50) values of 0.23 μM, measured after 7 days of treatment in MLL leukemia cells. MI-463 is effective in inducing differentiation of MLL leukemia cells. Treatment with sub-micromolar concentrations of MI-463 also leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of MLL fusion proteins substantially upregulated in MLL leukemias[1].

In vivo MI-463 shows substantial survival benefit in mouse models of MLL leukemia. It has very favorable druglike properties, including metabolic stability and PK profile in mice. MI-463 achieves high levels in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability(∼45%). In a mouse xenograft model using MV4;11 human MLL leukemia cells implanted into BALB/c nude mice, MI-463 induces strong inhibition of tumor growth with once-daily intraperitoneal (i.p.) administration. It does not impair normal hematopoiesis in vivo[1].

Protocol

Cell Research:[1]
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  • Cell lines: leukemia cells
  • Concentrations: --
  • Incubation Time: 6 or 7 days
  • Method: For viability assays, leukemia cells are plated at relevant concentrations and treated with compounds or 0.25% DMSO and cultured at 37°C for 7 days. Medium is changed at day 4, viable cell numbers are restored to the original concentration, and compounds are re-supplied. The MTT cell proliferation assay kit (Roche) is then used, and plates are read for absorbance at 570 nm using a PHERAstar BMG microplate reader. Effect of menin-MLL inhibitors on expression level is assessed by qRT-PCR after 6 days of incubation of compounds with cells, with medium changed and compound re-supply at day 3. For cell differentiation studies, leukemia cells are treated with menin-MLL inhibitors for 7 days, then harvested, washed, and incubated with Pacific Blue rat anti-mouse CD11b antibody before being analyzed by flow cytometry.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: C57BL/6 mice
  • Formulation: 25% (v/v) DMSO, 25% (v/v) PEG-400 and 50% (v/v) PBS
  • Dosages: 15 mg/kg
  • Administration: I.V.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (198.12 mM)
Ethanol 22 mg/mL (45.4 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 484.54
Formula

C24H23F3N6S

CAS No. 1628317-18-9
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID