AKI603

AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells[1][2].

Product Specifications

CAS Number

[1432515-73-5]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

Aurora Kinase

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/aki603.html

Purity

98.03

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

O=[N+]([O-])C1=CC=C(C=C1)NC2=NC(N3CCN(CC3)C)=CC(NC4=NNC(C)=C4)=N2

Molecular Formula

C19H23N9O2

Molecular Weight

409.45

Precautions

H315, H319, H320

References & Citations

[1]Le-Xun Wang, et al. Aurora A Kinase Inhibitor AKI603 Induces Cellular Senescence in Chronic Myeloid Leukemia Cells Harboring T315I Mutation. Sci Rep. 2016 Nov 8;6:35533.|[2]Fei-Meng Zheng, et al. A novel small molecule aurora kinase inhibitor attenuates breast tumor-initiating cells and overcomes drug resistance. Mol Cancer Ther. 2014 Aug;13 (8) :1991-2003.|[3]Zhenzhen Zhao, et al. Determination of a novel Aurora-A (AurA) kinase AKI603 by UPLC-MS/MS and its application to a bioavailability study in rat. J Pharm Biomed Anal. 2016 Jun 5;125:303-9.