1-(2-Chloroethyl)-3-(2,6-dioxo-3-piperidinyl)-1-nitrosourea

Water < 1 (mg/mL)

Water pH 4 < 1 (mg/mL)

Water pH 9 2-3 (mg/mL)

10% EtOH < 1 (mg/mL)

95% EtOH 2-3 (mg/mL)

McOH 3-4 (mg/mL)

Bulk: A sample stored at 60° C for 10 days decomposed 18% (UV). The compound was found to be stable in bulk form at room temperature exposed to lab light through 60 days (UV, TLC and ionic chloride). For long -term storage the bulk compound should be protected from moisture and stored at -15° C. Solution: The compound dissolved in 3% methanol/ water decomposed 4% in one hour, 6.5% in three hours 15% in six hours, and 38% in 24 hours (UV). There was no formation of ionic chloride during the 24 hours. Solutions should be prepared immediately before use.

Mouse(po): LD50 35700 lug/kg

Mouse(iv): LD50 22 mg/kg

Dog(iv): LDLo, 3 mg/kg

Monkey(iv): LDLo 10 mg/kg

A class of drugs that differs from other alkylating agents used clinically in that they are monofunctional and thus unable to cross-link cellular macromolecules. Among their common properties are a requirement for metabolic activation to intermediates with antitumor efficacy and the presence in their chemical structures of N-methyl groups, that after metabolism, can covalently modify cellular DNA. The precise mechanisms by which each of these drugs acts to kill tumor cells are not completely understood. (From AMA, Drug Evaluations Annual, 1994, p2026)