6553. Nimustine
Nomenclature
CAS number: 42471-28-3
N′-[(4-Amino-2-methyl-5-pyrimidinyl)methyl]-N-(2-chloroethyl)-N-nitrosourea. C9H13ClN6O2; mol wt 272.69.
C 39.64%, H 4.81%, Cl 13.00%, N 30.82%, O 11.73%.
Description and references
Chloroethylnitrosourea derivative with antitumor activity. Prepn: H. Nakao et al., DE 2257360; eidem, US 4003901 (1973, 1977 both to Sankyo); eidem, Yakugaku Zasshi 94, 1932 (1974), C.A. 82, 43263y (1975). Effects on macrophage cytostatic activity in rats: N. Saijo et al., Br. J. Cancer 42, 162 (1980). Distribution, excretion, metabolism in mice: M. Tanaka et al., Cancer Treat. Rep. 64, 575 (1980). Exptl and clinical effect: N. Saijo et al., Cancer Chemother. Pharmacol. 4, 165 (1980). Acute toxicity: H. Masuda et al., Sankyo Kenkyusho Nempo 29, 118 (1977), C.A. 88, 146298s (1978).
Properties
Pale yellow crystals from ethanol, dec 125°.Derivative
Hydrochloride.Nomenclature
CAS number: 55661-38-6
NSC-245382; ACNU (Baxter); Nidran (Sankyo). C9H13ClN6O2.HCl; mol wt 309.15.
C 34.97%, H 4.56%, Cl 22.94%, N 27.18%, O 10.35%.
Properties
White to light yellow cryst powder. uv max (0.04N HCl): 245 nm (E1%1cm 480-510). Sol in methanol, slightly sol in abs ethanol, n-butanol. Practically insol in ethyl acetate, ether, chloroform, benzene, n-hexane. Gradually develops greenish yellow color in light; decomposes slowly in humid air. LD50 in mice, rats (mg/kg): 62, 46 i.v. (Masuda).Therapeutic Category
Antineoplastic.
Keywords
Antineoplastic; Alkylating Agents; Nitrosoureas