Melting Point: 214°C (alternatively, 189-195°C with decomposition during melting; or 197-198°C)
Boiling Point: 545.7±60.0°C at 760 mmHg
Flash Point: 283.8±32.9°C
Density: 1.9±0.1 g/cm3
Vapor Pressure: 0.0±3.2 mmHg at 25°C
Solubility: Highly soluble in water (up to 48 mg/mL or 100mM), soluble in DMSO (up to 50mM), slightly soluble in methanol and ethanol, practically insoluble in ether
Storage Conditions: Store at 2-8°C; once dissolved in solvent, store at -20°C and use within one month (alternatively, store at -20°C with a shelf life of 2 years)
Chemical and Biochemical Properties
Category: Nucleoside analog, antimetabolite
Mechanism of Action: Phosphorylated to the triphosphate form (Ara-CTP), which competes with dCTP for incorporation into DNA, blocking DNA synthesis by inhibiting the function of DNA and RNA polymerases
IC50 Value: IC50 for inhibiting DNA synthesis is 16 nM
Biological Activity: Causes S-phase cell cycle arrest and exhibits antiviral (HSV) and anti-orthopoxvirus activity
Pharmacological Effects
Antitumor Effects: The primary mechanism is competitive inhibition of DNA polymerase and incorporation into DNA chains, terminating DNA activity. It is a potent inhibitor of DNA replication and is highly effective in treating acute leukemia, including acute lymphocytic leukemia and non-lymphocytic leukemia, as well as malignant lymphomas.
Cytotoxicity: Ara-CTP can also alter intracellular phospholipid and glycoprotein metabolism, leading to cytotoxic effects.
