An inhibitor of the MDM2 and p53 interaction (KD = 0.045 nM; IC50 = 0.6 nM in a cell-free binding assay); inhibits proliferation of HCT116 p53 wild-type

AMG 232 – 5 mg

Brand:
Cayman
CAS:
1352066-68-2
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An inhibitor of the MDM2 and p53 interaction (KD = 0.045 nM; IC50 = 0.6 nM in a cell-free binding assay); inhibits proliferation of HCT116 p53 wild-type, but not p53-/-, cells (IC50s = 10 nM and >25 µM, respectively); reduces tumor growth in an SJSA-1 osteosarcoma mouse xenograft model (ED50 = 9.1 mg/kg); induces complete regression of tumors in an SJSA-1 osteosarcoma mouse xenograft model at 75 mg/kg per day for 10 days; induces apoptosis of SJSA-1 mouse xenograft tumor cells

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

Synonyms: 

Molecular weight: 568.6

CAS: 1352066-68-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53

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