Description
An inhibitor of the MDM2-p53 interaction (IC50 = 1.7 nM for human MDM2 in a TR-FRET assay); selective for human MDM2 (Ki = 1.3 nM) over dog, mouse, and rat Mdm2 (Kis = 20.5, 65.9, and 47.4 nM, respectively); selectively inhibits proliferation of AML cells expressing wild-type p53 (IC50s = 50-1,000 nM) over AML cells expressing mutant p53 (IC50s = >1,000 nM); induces tumor regression in a PDX mouse model of AML at 100 mg/kg per day
Formal name: (1S)-1-(4-chlorophenyl)-1,4-dihydro-6-methoxy-7-(1-methylethoxy)-2-[4-[methyl[[trans-4-(4-methyl-3-oxo-1-piperazinyl)cyclohexyl]methyl]amino]phenyl]-3(2H)-isoquinolinone
Synonyms:
Molecular weight: 659.3
CAS: 1313363-54-0
Purity: ≥98%
Formulation: A crystalline solid
