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MI-463

Catalog No. TQ0058 CAS 1628317-18-9

MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).

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MI-463, CAS 1628317-18-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 55.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 278.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 538.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 100%

Purity: 99.28%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MI-463 is a potent and orally bioavailable inhibitor of the menin-mLL interaction (IC50: 15.3 nM).
In vitro	Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-463 results in substantial growth inhibition (GI50: 0.23 μM). 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.
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 level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (45%). MI-463 induces strong inhibition of tumor growth with once-daily intraperitoneal (i.p.) administration. The expression of mLL fusion protein target genes, HOXA9 and MEIS1, is significantly reduced upon treatment with MI-463.
Cell Research	Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed on day 4, viable cell numbers are restored to the original concentration and MI-463 is re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader.
Animal Research	For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×10^6 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm^3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or MI-463 are administrated once daily at designated doses using i.p. injections.

Molecular Weight	484.54
Formula	C24H23F3N6S
CAS No.	1628317-18-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL (247.66 mM), Sonication is recommended.

References and Literature

1. Borkin D, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27(4):589-602.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Histone Modification Compound Library Epigenetics Compound Library Reprogramming Compound Library Stem Cell Differentiation Compound Library Chromatin Modification Compound Library Covalent Inhibitor Library Anti-Aging Compound Library Orally Active Compound Library

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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

MI-463 1628317-18-9 Chromatin/Epigenetic Epigenetic Reader Domain Histone Methyltransferase Inhibitor MI 463 inhibit MI463 inhibitor

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