[CAS NO. 1246529-32-7] MPI-0479605

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PRODUCTS SPECIFICATIONS [1246529-32-7]

Catalog

SLK-S7488

Brand

Selleck

CAS

1246529-32-7

DESCRIPTION [1246529-32-7]

Overview

MDL	MFCD28099811
Molecular Weight	407.51
Molecular Formula	C22H29N7O
SMILES	CC1=CC(N2CCOCC2)=CC=C1NC3=NC(NC4CCCCC4)=C5N=CNC5=N3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.4539 mL	12.2696 mL	24.5393 mL
5 mM	0.4908 mL	2.4539 mL	4.9079 mL
10 mM	0.2454 mL	1.2270 mL	2.4539 mL
50 mM	0.0491 mL	0.2454 mL	0.4908 mL

Description

MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase with of 1.8 nM, >40-fold selectivity over other kinases.

Targets

Mps1 ^[1]

1.8 nM

In vitro

MPI-0479605 impairs the SAC and the bipolar attachment of chromosomes to the mitotic spindle, which results in chromosome segregation defects and aneuploidy. MPI-0479605 results in a significant decrease in cell viability with GI50 ranging from 30 to 100 nM in a panel of tumor cell lines. In addition, MPI-0479605 also causes cell growth arrest and ultimately promotes cell death by apoptosis or mitotic catastrophe.

In vivo

MPI-0479605 (30 mg/kg daily or 150 mg/kg every 4 days, i.p.) shows antitumor activity in colon cancer xenograft models.

References

[1] Tardif KD, et al. Mol Cancer Ther. 2011, 10(12), 2267-2275.