Molecular Formula | C9H15NO3
|
Molar Mass | 185.22 |
Density | 1.32±0.1 g/cm3(Predicted) |
Melting Point | 146-147 °C |
Boling Point | 353.7±17.0 °C(Predicted) |
Water Solubility | Soluble in water at 10mg/ml |
Solubility | H2O: >10mg/mL |
Appearance | solid |
Color | white to off-white |
pKa | 13.68±0.10(Predicted) |
Storage Condition | Inert atmosphere,2-8°C |
Sensitive | Light Sensitive |
In vitro study | PRIMA-1 is converted to a thiol adduct-forming compound in p53 mutants. PRIMA-1 modifies the thiol group of the p53 mutant to restore its tumor suppressor activity. PRIMA-1 inhibits the growth of pancreatic cancer cells, induces cell cycle arrest and reduces DNA synthesis. It can selectively induce apoptosis and cell death in pancreatic cancer cells expressing p53 mutants, and activate p53-dependent apoptotic pathways. PRIMA-1 enhances the cytotoxicity of chemotherapeutic drugs on p53 mutant pancreatic cancer cells. PRIMA-1 has high antileukemic activity in NB4 cells derived from acute promyelocytic leukemia. The apoptosis induced by PRIMA-1 was time-dependent and dose-dependent. The apoptosis caused by it is related to the activation of caspase-9, caspase-7 and PARP fragmentation. PRIMA-1 had no significant apoptotic effect on normal human peripheral blood mononuclear cells. |
In vivo study | The mice were injected intravenously, and the injection of PRIMA-1 did not result in any significant weight and behavioral differences (compared to the control group). In a mouse tumor model, PRIMA-1 has antitumor activity and is capable of p53 mutant-dependent tumor growth. |