MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor ( IC 50 =4.4 nM; K i =0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
In Vitro
MI-1061 achieves IC 50 =100 and 250 nM in the SJSA-1 and HCT-116 p53 +/+ cell lines, respectively, and has IC 50 >10000 nM in the p53 knockout cell line HCT-116 p53 –/– cell line. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MI-1061 (100 mg/kg; p.o.; daily for 14 days) is capable of achieving tumor regression in the SJSA-1 xenograft tumor model in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice bearing SJSA-1 osteosarcoma xenografts Dosage: 100 mg/kg Administration: P.o.; daily for 14 days Result: Demonstrated strong antitumor activity and achieved significant tumor regression.
