Danusertib (PHA-739358) is a potent, ATP-competitive Aurora kinase inhibitor with IC50 of 13,79 and 61 nM for Aurora A, B and C, respectively.
Danusertib (PHA-739358) also inhibits Abl, RET, and FGFR1 (IC50=25,31, and 47 nM), efficiently inhibits imatinib-resistant Abl mutant T315I (IC50=5 nM)。
Danusertib (PHA-739358) inhibits phosphorylation of histone H3 in Ser10, and has significant antitumor activity in different xenografts and spontaneous and transgenic animal tumor models.
