For research use only.

Catalog No.S7816

1 publication

MI-463 Chemical Structure

CAS No. 1628317-18-9

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

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Selleck's MI-463 has been cited by 1 publication

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


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
  • 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


CAS No. 1628317-18-9
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C=CC2=C1C=C(N2)C#N)CN3CCC(CC3)NC4=C5C=C(SC5=NC=N4)CC(F)(F)F

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID