Title: Lomustine
CAS Registry Number: 13010-47-4
CAS Name: N-(2-Chloroethyl)-N¢-cyclohexyl-N-nitrosourea
Additional Names: 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea
Manufacturers' Codes: NSC-79037; RB-1509
Trademarks: Belustine (Bellon); CCNU (Lundbeck); Cecenu (Medac); CeeNU (BMS); CiNU (BMS)
Molecular Formula: C9H16ClN3O2
Molecular Weight: 233.70
Percent Composition: C 46.25%, H 6.90%, Cl 15.17%, N 17.98%, O 13.69%
Literature References: Chloroethylnitrosourea derivative with antitumor activity. Similar to carmustine, chlorozotocin, nimustine, ranimustine, q.q.v. Synthesis: T. P. Johnston et al., J. Med. Chem. 9, 892 (1966). Clinical review: S. K. Carter, J. W. Newman, Cancer Chemother. Rep. Part 3 1, 136 (1968). Physiological disposition: V. T. Oliverio et al., Cancer Res. 30, 1330 (1970). Toxicology and pharmacology: G. R. Thompson, R. E. Larson, Toxicol. Appl. Pharmacol. 21, 405 (1972); V. T. Oliverio, Cancer Chemother. Rep. Part 3 4, 13 (1973). Comprehensive description: F. J. Al-Shammary, Anal. Profiles Drug Subs. 19, 315-340 (1990).
Properties: Yellow powder, mp 90°. Freely sol in chloroform; sol in ethanol, acetone. Soly in water, 0.1N NaOH, 0.1N HCl or 10% ethanol: <0.05 mg/ml; in absolute ethanol: 70 mg/ml. The bulk drug should be stored in a deep freeze and protected from moisture. LD50 in male mice (mg/kg): 51 orally; 56 i.p.; 61 s.c. (Thompson, Larson).
Melting point: mp 90°
Toxicity data: LD50 in male mice (mg/kg): 51 orally; 56 i.p.; 61 s.c. (Thompson, Larson)
CAUTION: This substance is reasonably anticipated to be a human carcinogen: Report on Carcinogens, Eleventh Edition (PB2005-104914, 2004) p III-52.
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Alkylating Agents; Nitrosoureas. |