Back to products

Browse products

MedKoo product information:

R763

Description of R763 (formerly AS703569): R763 is an orally bioavailable, synthetic, small-molecule multi-Aurora kinase inhibitor with potential antineoplastic activity. Aurora kinase inhibitor R763 selectively binds to and inhibits multiple Aurora kinases (AKs), which may result in the inhibition of cell division and proliferation, and the induction of apoptosis in tumor cells that overexpress AKs. Overexpressed in certain tumor cell types, AKs, a family of serine-threonine kinases, are important regulators of cell division and proliferation that are involved in controlling chromatid segregation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Current developer:    Merck Serono S.A., Switz.  

R763/AS703569 inhibits Aurora kinases, along with a limited no. of other kinases including FMS-related tyrosine kinase 3 (FLT3), and has potent anti-proliferative activity against many cell types accompanying unique phenotypic changes such as enlarged cell size, endoreduplication and apoptosis. The endoreduplication cycle induced by R763/AS703569 was irreversible even after the compd. was withdrawn from the culture. Oral administration of R763/AS703569 demonstrated marked inhibition of tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia. An acute myeloid leukemia cell line MV4-11, which carries a FLT3 internal tandem duplication mutation, is particularly sensitive to R763/AS703569 in vivo. Conclusions R763/AS703569 is a potent inhibitor of Aurora kinases and exhibited significant anti-proliferative activity against a wide range of tumor cells both in vitro and in vivo. Inhibition of Aurora kinases has the potential to be a new addn. to the treatment of cancers.  see Journal of Cancer Research and Clinical Oncology (2010), 136(1), 99-113

 1. Martinelli, Giovanni; Iacobucci, Ilaria; Papayannidis, Cristina; Soverini, Simona. New targets for Ph+ leukaemia therapy. Best Practice & Research, Clinical Haematology (2009), 22(3), 445-454.

2. McLaughlin, John; Markovtsov, Vadim; Li, Hui; Wong, Steve; Gelman, Marina; Zhu, Yanhong; Franci, Christian; Lang, D. Wayne; Pali, Erlina; Lasaga, Joe; Low, Caroline; Zhao, Feifei; Chang, Betty; Gururaja, Tarikere L.; Xu, Weiduan; Baluom, Muhammad; Sweeny, David; Carroll, David; Sran, Arvinder; Thota, Sambaiah; Parmer, Manjeet; Romane, Angela; Clemens, George; Grossbard, Elliott; Qu, Kunbin; Jenkins, Yonchu; Kinoshita, Taisei; Taylor, Vanessa; Holland, Sacha J.; Argade, Ankush; Singh, Rajinder; Pine, Polly; Payan, Donald G.; Hitoshi, Yasumichi. Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. Journal of Cancer Research and Clinical Oncology (2010), 136(1), 99-113. 

3. Romanelli, Angela; Gianella-Borradori, Athos; Raymond, Eric; Serova, Maria; Faivre, Sandrine. Antitumor combinations of (1R,2R,3S,4S)-N4-(3-aminocarbonylbicyclo[2.2.1]hept-5-en-2-yl)-5-fluoro-N2-[(3-methyl-4-(4-methylpiperazin-1-yl]phenyl-2,4-pyrimidinediamine and signaling inhibitors. PCT Int. Appl. (2009), 45pp. CODEN: PIXXD2 WO 2009050143 A1 20090423 

4. Martinelli Giovanni; Iacobucci Ilaria; Papayannidis Cristina; Soverini Simona New targets for Ph+ leukaemia therapy. Best practice & research. Clinical haematology (2009), 22(3), 445-54.