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| | NVP-CGM097 Basic information |
| Product Name: | NVP-CGM097 | | Synonyms: | NVP-CGM097;CGM097;CS-1248;CS-2423;CGM097; CGM-097; CGM 097; NVPCGM097; NVPCGM 097; NVPCGM-097;(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;NVP-CGM097 (CGM097);(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 | | CAS: | 1313363-54-0 | | MF: | C38H47ClN4O4 | | MW: | 659.26 | | EINECS: | | | Product Categories: | | | Mol File: | 1313363-54-0.mol |  |
| | NVP-CGM097 Chemical Properties |
| 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) | | pka | 8.31±0.20(Predicted) | | form | Powder |
| | NVP-CGM097 Usage And Synthesis |
| 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 |
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| | NVP-CGM097 Preparation Products And Raw materials |
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