Home Epigenetics Histone Methyltransferase inhibitor - MLL inhibitor MI-463

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MI-463 Histone Methyltransferase inhibitor

Cat.No.S7816

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

Chemical Structure

Molecular Weight: 484.54

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Quality Control

Batch: S781601 DMSO]96 mg/mL]false]Ethanol]22 mg/mL]false]Water]Insoluble]false Purity: 99.83%
99.83

Chemical Information, Storage & Stability

Molecular Weight 484.54 Formula

C24H23F3N6S

 Storage (From the date of receipt)
CAS No. 1628317-18-9 Download SDF Storage of Stock Solutions

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

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (198.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Menin-MLL interaction [1]
(Cell-free assay)
15.3 nM
In vitro
MI-463 demonstrates profound on-target activity in MLL leukemia cells. This compound 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. It is effective in inducing differentiation of MLL leukemia cells. Treatment with sub-micromolar concentrations of this chemical 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. This compound 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, this chemical induces strong inhibition of tumor growth with once-daily intraperitoneal (i.p.) administration. It does not impair normal hematopoiesis in vivo[1].
References

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