| Identification | Back Directory | [Name]
NVP-CGM097 | [CAS]
1313363-54-0 | [Synonyms]
CGM097
CS-1248
CS-2423
NVP-CGM097
NVP-CGM097 (CGM097)
CGM097; CGM-097; CGM 097; NVPCGM097; NVPCGM 097; NVPCGM-097
(S)-1-(4-Chlorophenyl)-7-isopropoxy-6-methoxy-2-(4-[methyl[4-(4-methyl-3-oxopiperazin-1-yl)-trans-cyclohexylmethyl]amino]phenyl)-1,4-dihydro-2H-isoquinolin-3-one
(S)-1-(4-Chlorophenyl)-7-isopropoxy-6-methoxy-2-(4-(methyl(((1r,4S)-4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl)methyl)amino)phenyl)-1,2-dihydroisoquinolin-3(4H)-one
3(2H)-Isoquinolinone, 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]-, (1S)-
(S)-1-(4-chlorophenyl)-7-isopropoxy-6-methoxy-2-(4-(methyl(((1r,4r)-4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl)methyl)amino)phenyl)-1,2-dihydroisoquinolin-3(4H)-one hydrochloride | [Molecular Formula]
C38H47ClN4O4 | [MDL Number]
MFCD28144684 | [MOL File]
1313363-54-0.mol | [Molecular Weight]
659.26 |
| Chemical Properties | Back Directory | [Boiling point ]
830.1±65.0 °C(Predicted) | [density ]
1.210±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:50.0(Max Conc. mg/mL);75.84(Max Conc. mM) | [form ]
Powder | [pka]
8.31±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Biological Activity]
NVP-CGM097 is a potent and selective MDM2 inhibitor with a Ki value of 1.3 nM. It binds to the p53-binding site of the MDM2 protein, disrupting its protein-protein interactions, leading to activation of the p53 pathway. | [in vitro]
The binding ability of NVP-CGM097 to MDM2 varies among different species. The selectivity of it for p53:MDM2 interaction is 1176-fold for p53:MDM4 interaction, 3000-fold for Ras:Raf interaction, and 1176-fold for Bcl-2:Bak, Bcl-2:Bad, Mcl- The interaction of 1:Bak, Mcl-1:NOXA, XIAP:BIR3, c-IAP:BIR3 is inactive, therefore, it is highly selective for p53:MDM2. It can significantly promote the entry of wild-type p53 into the nucleus with IC50 of 0.224 μM, indicating that it can inhibit the p53:MDM2 interaction in living cells. It promotes p53 as nucleus, resulting in cellular p53-dependent growth inhibition. | [in vivo]
After intravenous injection, the serum clearance of NVP-CGM097 was 5 mL/min/kg in mice, 7 mL/min/kg in rats, 3 mL/min/kg in dogs, and 3 mL/min/kg in monkeys. 4 mL/min/kg. Serum clearance of NVP-CGM097 was low in all species compared to hepatic blood flow (typically 5-10% hepatic blood flow). The half-life of NVP-CGM097 in rodents and monkeys is 6-12 hours; in dogs, the half-life is 20 hours, which is relatively longer. | [target]
| Target | Value | hMDM2
(Cell-free assay) | 1.7 nM |
| [storage]
Store at -20°C |
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