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Background Information:
NVP-CGM097 (CGM-097) is a potent and selective MDM2 inhibitor. Optically pure (S-Enantiomer) NVP-CGM097 binds to the p53 binding-site of the Human MDM2 protein with an IC50 value of 1.7 nM, highly selective against other protein-protein interactions such as p53:MDM4 (>1000-fold selectivity), Ras:Raf (3000-fold selectivity), and showing no signi?cant activity against Bcl-2:Bak, Bcl-2:Bad, Mcl-1:Bak, Mcl-1:NOXA, XIAP:BIR3, and c-IAP:BIR3 protein−protein interactions. It inhibits the p53:MDM2 interaction in cells, leading to p53 nuclear translocation that results in cell growth inhibition in a p53-dependent manner (ref. 1). Exhibit excellent in vivo pharmacological properties. It is currently in clinical evaluations in p53wt tumors (ref. 1).
Reference:
1. P. Holzer, et al, Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase1 Clinical Trials in p53wt Tumors, J. Med. Chem. 2015, 58, 6348−6358.
APIM050306: NVP-CGM097 (FREE BASE)
CAS No.: 1313363-54-0.
Molecular Formula: C38H47ClN4O4.
Molecular Weight: 659.3 (refer to Certificate of Analysis, batch-specific).
Purity: >99% (by achiral HPLC), 100% optically pure (by chiral HPLC).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Elemental Analysis Report.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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