NVP-CGM097
- CAS NO.:1313363-54-0
- Empirical Formula: C38H47ClN4O4
- Molecular Weight: 659.26
- MDL number: MFCD28144684
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:03
What is NVP-CGM097?
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.
Properties of NVP-CGM097
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 |
Safety information for NVP-CGM097
Computed Descriptors for NVP-CGM097
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