Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.

Lomustine对ZR-75-1和U373的生长具有抑制作用，其IC50分别为12 μM和15 μM。Lomustine降低DNA修复蛋白O6-alkylguanine-DNA alkyltransferase的表达水平。[1] Lomustine (420 μM)通过降低抗凋亡蛋白Bcl-2和Bcl-xl的水平，分别在小脑星形细胞瘤细胞、正常人上皮细胞和成纤维细胞中触发通过线粒体途径的凋亡。Lomustine在小脑星形细胞瘤细胞中引起G2/M期的细胞周期延迟，并在HFSN1细胞中以p53独立的方式上调p21蛋白水平。[2]

Lomustine可导致延迟性、累积剂量相关的慢性肝毒性，此种肝毒性是不可逆转的且可能致命。[4] 在自发生长肿瘤的猫中，Lomustine可能引起罕见的严重血液学毒性，其III级或IV级中性粒细胞减少症和血小板减少症的发生率分别为4.1%和1.0%。在自发生长肿瘤的猫中，Lomustine倾向于导致进展性中性粒细胞减少症的可能性更大，并且在统计学上显著提高了响应率。[5]

Cell lines are routinely grown as monolayers in DMEM supplemented with 10% foetal calf serum, 25 mm HEPES, glutamine and penicillin/streptomycin. Cytotoxicity studies are carried out in HEPES-free medium in a 5% CO2 atmosphere. 750-1000 cells/well are plated in 96 well plates and after overnight incubation are treated for 2 hours with or without 33 μM BG. Temozolomide or CCNU is then added for 1 hour in the same medium, the final DMSO concentration not exceeding 1%. The cells are grown for a further 7 days in fresh medium and assayed for protein content by the NCI sulphorhodamine assay; growth studies show that cells are in log phase growth during the assay period. For the repeat temozolomide dosing schedule cells are given consecutive 24 hours treatments, with fresh medium each day. Assays are carried out at least in duplicate.(Only for Reference)