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.
性状
Solid
体外研究(In Vitro)
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 p53cell line. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: SCID
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Aguilar A, et al. Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannich ring-opening-cyclization reaction mechanism in spiro-oxindoles. J Med Chem. 2014;57(24):10486-10498.
溶解度数据
In Vitro: DMSO : 120 mg/mL (172.30 mM; Need ultrasonic)配制储备液