NVX-207
Names
[ CAS No. ]:
745020-66-0
[ Name ]:
NVX-207
[Synonym ]:
2-Amino-3-hydroxy-2-(hydroxymethyl)propyl (3β)-3-acetoxylup-20(29)-en-28-oate
Lup-20(29)-en-28-oic acid, 3-(acetyloxy)-, 2-amino-3-hydroxy-2-(hydroxymethyl)propyl ester, (3β)-
Biological Activity
[Description]:
NVX-207 is a derivative of betulinic acid with anti-cancer activity.
[Related Catalog]:
[In Vitro]
NVX-207 shows anti-tumour activity (mean IC50 = 3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of poly (ADP-ribose) polymerase (PARP). NVX-207 induces cell death via apoptosis[1]. NVX-207 has a high cytotoxicity with IC50 values ranging from 7.6-8.5 µM, in the three analyzed malignant glioma cell lines. NVX-207 leads to PARP cleavage and to a decrease in Survivin expression levels under normoxic and hypoxic conditions. NVX-207 (20 µM) causes a significantly high rate of necrosis of glioma cell lines[2].
[In Vivo]
Intravenous application of NVX-207 in mice is well tolerated[1].
[Cell Assay]
Cytotoxic activities are evaluated using the Sulforhodamine-B (SRB) assay. Exponentially growing cells are seeded into 96-well plates at cell densities to prevent confluence for 96 h. After 24 h, the cells are treated using a dilution series of the compounds for 72 h under normoxic or hypoxic conditions. After treatment, the adherent cells are fixed using 10% TCA at 4°C for 1 h; the cells are washed with ice-cold water and are dyed using 100 µL of 4.4% SRB solution for 10 min. After staining, the plates are washed with 1% acetic acid and air-dried overnight. Three hundred microliters of 20 mM Tris base solution is added, and the absorbance is measured at 540 nm using a 96-well plate reader. The IC50 values indicate the concentrations of the compound that cause 50% cell inhibition. The data are obtained in three independent experiments.
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Density]:
1.1±0.1 g/cm3
[ Boiling Point ]:
664.8±55.0 °C at 760 mmHg
[ Molecular Formula ]:
C36H59NO6
[ Molecular Weight ]:
601.857
[ Flash Point ]:
355.8±31.5 °C
[ Exact Mass ]:
601.434265
[ LogP ]:
9.76
[ Vapour Pressure ]:
0.0±4.6 mmHg at 25°C
[ Index of Refraction ]:
1.553
[ Storage condition ]:
2-8℃