MI-463 Inhibitor

Name: MI-463 Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5764316
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5764316

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

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

MI-463, Inhibitor

Full Product Name

MI-463

Product Gene Name

MI-463, inhibitor

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

484.54

Solubility

DMSO: 120mg/mL (247.66mM) Need ultrasonic
Water: Insoluble
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C24H23F3N6S

SMILES

CC1=C2C=C(NC2=CC=C1CN1CCC(CC1)NC1=NC=NC2=C1C=C(CC(F)(F)F)S2)C#N

CAS Number

1628317-18-9

Cell Research

Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 degree 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 570nM using a microplate reader.

In Vitro

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.

Product Categories/Family for MI-463, inhibitor

Chromatin/Epigenetic; Histone Methyltransferase

Product References and Citations for MI-463, inhibitor

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.

Other Notes

Small volumes of MI-463, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for MI-463 purchase

MBS5764316 is an inhibitor targeting MI-463.