产品属性:
产品名称
规格
CAS号
型号
AM-8735
250mg 500mg
1429386-01-5
EY-Y0163785
Cas No.1429386-01-5
别名 N/A
化学名 N/A
分子式 C27H31Cl2NO6S
分子量 568.51
溶解度 Soluble in DMSO
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: AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM.
AM-8735 displays substantial growth inhibition of wild-type p53 cells (IC50=63 nM) and no growth inhibition of p53-deficient cells (IC50>25 μM). AM-8735exhibits a dose-dependent increase of p21 mRNA, a direct transcriptional readout of p53 activity, in HCT116 p53wt cells (IC50=160 nM)[1].
AM-8735 also demonstrates significant time and concentration dependent p21 mRNA induction in vivo in a pharmacodynamic assay in SJSA-1 osteosarcoma tumors. AM-8735 shows excellent antitumor activity in the SJSA-1 osteosarcoma xenograft model with an ED50 of 41 mg/kg[1].
[1]. Gonzalez AZ, et al. Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction. J Med Chem. 2014 Mar 27;57(6):2472-88.
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