Chemren Bio-Engineering Co., Ltd.

Description of:Danusertib(PHA-739358)
PHA-739358 is a pyrrolo-pyrazole, which inhibits Aurora kinases in a biochemical assay with IC50s of 13, 79, and 61 nmol/L for Aurora A, B, and C, respectively. High activity was also observed against other kinases: Ret, Trk-A, and Abl (~2-fold higher IC50 compared with Aurora A), FGFR-1(4-fold higher IC50 compared with Aurora A).Several tumor cell lines (including colon, breast, prostate, lung, and ovary) were exposed to PHA-739358 and cell IC50 was in the range of 28 nmol/L (A2780) up to 300 nmol/L (U2OS).The compound has good PK properties and a strong antitumor activity observed in a broad range of in vivo tumor models with minor and transient toxicity signs.