Biological Activity:
AZD1152 was shown to be effective on SW620 tumors in nude mice after a single dose resulted in significant and durable inhibition of tumor growth; as a result this compound has been selected for clinical evaluation. AZD1152 is 1000-fold more selective for aurora kinase B than for aurora kinase A with Ki values of 1300 nM and 0.36 nM for aurora kinase A and B, respectively. AZD1152-HQPA, at concentrations as low as 0.01 µM, produced a significant (p£¼0.05) decrease in the ability of NB4 cells to proliferate by 48 hours.
Related Compounds:
S1048 VX-680 (MK-0457) :Aurora kinase, Flt-3, Abl Inhibitor.
S1100 MLN8054 :An orally bioavailable, highly selective Aurora Kinase inhibitor.
S1103 ZM-447439:A potent inhibitor of Aurora-B (IC50 50 nM).
S1107 PHA739358(Danusertib) :Inhibitor of Aurora kinases,Bcr-Abl and FGFR.
S1133 MLN8237 :Aurora kinase inhibitor
S1134 AT9283 :Aurora kinases Inhibitor
Technical Data:
M.Wt: 507.56
Formula: C26H30FN7O3
Solubility: Soluble in DMSO
Purity: 99%
Storage: -20C 2 years
CAS No: 722544-51-6
References:
1. Mortlock AA, Foote KM, Heron NM, Jung FH, Pasquet G, Lohmann JJ, et al. Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of Aurora B Kinase. J Med Chem 2007; 50:2213-24.
2. Keen N, Brown E, Crafter C, Wilkinson R, Wedge S, Foote KM, et al. Biological characterisation of AZD1152, a highly potent and selective inhibitor of Aurora kinase activity. AACR-NCI-EORTC International Conference. Molecular Targets and Cancer Therapeutics. 14-18 November 2005. Philadelphia, PA, USA.
3. Walsby E, Walsh V, Pepper C, Burnett A, Mills K.. Effects of the aurora kinase inhibitors AZD1152-HQPA and ZM447439 on growth arrest and polyploidy in acute myeloid leukemia cell lines and primary blasts. Haematologica. 2008 May;93(5):662-9. Epub 2008 Mar 26.
