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

color 

Light yellow to yellow

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

NVP-CGM097(1313363-54-0)Related Product Information

• NVP-BAW2881
• BEZ235 (Tosylate)
• NVP-AAM077
• NVP-LDE225
• NVP-TNKS656
• TAE226 (NVP-TAE226)
• NVP-ADW742
• NVP-BEP800
• NVP-TAE684
• NVP-BEZ 235
• LMI070
• N-(3-Bromo-4-methylphenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine
• NVS-PAK1-1
• NVP-BSK805
• NVP BGJ398 phosphate
• Infigratinib
• 3-amino-N-(3-(4-amino-4-methylpiperidin-1-yl)pyridin-2-yl)-6-(3-(trifluoromethyl)pyridin-2-yl)pyrazine-2-carboxamide