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RO5353 is a potent and orally active p53-MDM2 inhibitor. The development of small-molecule MDM2 inhibitors to restore dysfunctional p53 activities represents a novel approach for cancer treatment.

RO5353 is an orally active inhibitor for p53-MDM2 with an IC50 of 7 nM for MDM2. RO5353 inhibits the proliferation of wild-type p53 cancer cells with an average IC50 of 7 nM. RO5353 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice[1].

[1] Zhang Z, et al., Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development. ACS Med Chem Lett. 2013 Dec 29;5(2):124-7. DOI:10.1021/ml400359z