Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: (3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-3-methyl-1-[(1S)-2-methyl-1-[[(1-methylethyl)sulfonyl]methyl]propyl]-2-oxo-3-piperidineacetic acid
Purity: ≥98%
Formula Markup: C28H35Cl2NO5S
Formula Weight: 568.55264
CAS Number: 1352066-68-2
Notes: AMG 232 is an inhibitor of the murine double minute 2 (MDM2) interaction with the tumor suppressor p53 (KD = 0.045 nM; IC50 = 0.6 nM in a cell-free binding assay).{48262} It inhibits proliferation of HCT116 p53 wild-type, but not p53-/-, cells (IC50s = 10 nM and >25 µM, respectively).{48263} It reduces tumor growth in an SJSA-1 osteosarcoma mouse xenograft model (ED50 = 9.1 mg/kg) and induces complete regression of tumors in the same model when administered at a dose of 75 mg/kg per day for 10 days.{48263,48262} It induces apoptosis of SJSA-1 mouse xenograft tumor cells, decreasing BrdU-labeled cells, increasing cleaved caspase-3, and halting the cell cycle.{48262}
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