MI-1061 是一种有效的，口服可生物利用的，化学稳定性的 MDM2 (MDM2-p53 互作) 抑制剂 (IC50=4.4 nM; Ki=0.16 nM)。MI-1061 能有效激活 p53，诱导细胞凋亡，并具有抗肿瘤活性。
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity[1]. IC50: 4.4 nM (MDM2)[1]Ki: 0.16 nM (MDM2)
MI-1061 achieves IC50=100 and 250 nM in the SJSA-1 and HCT-116 p53+/+ cell lines, respectively, and has IC50>10000 nM in the p53 knockout cell line HCT-116 p53-/-cell line[1].
MI-1061 is capable of achieving tumor regression in the SJSA-1 xenograft tumor model in mice with oral administration[1].
[1]. Aguilar A, et al. Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannichring-opening-cyclization reaction mechanism in spiro-oxindoles. J Med Chem. 2014 Dec 26;57(24):10486-98.
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