1309684-94-3

RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC₅₀ = 5 nM). It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC₅₀ value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.

RO 8994 is a potent and selective spiroindolinone MDM2 inhibitor, and potential useful for cancer therapy.

[1] ZHUMING ZHANG . Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy[J]. Bioorganic & Medicinal Chemistry, 2014, 22 15: Pages 4001-4009. DOI: 10.1016/j.bmc.2014.05.072