性能参数

产品名称

AM-8735

规格

250mg 500mg

货号

GOY-Y0555

 含量

>98.00%

CAS

1429386-01-5

别名

N/A

化学名

N/A

分子式

C27H31Cl2NO6S

分子量

分子 568.51

溶解度

Soluble in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

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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