1410737-34-6MI-1061

产品属性：

Cas No.1410737-34-6

别名 N/A

化学名 N/A

分子式 C30H26Cl2FN3O4

分子量 582.45

溶解度 DMSO: 300 mg/mL (515.07 mM)

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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.