NVP-CGM097 (FREE BASE)

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.