tcsc1461 Lomustine

Lomustine (CCNU) is a DNA alkylating agent, with antitumor activity.

IC50 & Target: DNA Alkylator^[1]

In Vitro: Lomustine (CCNU) is a DNA alkylating agent. Lomustine (CCNU, 0-250 μM) is cytotoxic to the U87-MG cells expressing tumor-derived mutant IDH1, and has little effect on the expression of wild-type IDH1. The combination of Lomustine and procarbazine or vincristine has no additive effect on the killing of cells expressing mutant or wild-type IDH1. Moreover, overexpression of either ALKBH2 or ALKBH3 partially reduces the death HT1080 cells exposed to Lomustine^[1]. Lomustine (CCNU) suppresses U87-MG growth with an ED50 of 68.1 μM. Lomustine (CCNU) (30, 40 μM) in combination with docosahexaenoic acid (DHA) darmatically inhibits 2 additional human-derived glioblastoma cell lines, and induces U87-MG apoptosis and necrosis. Lomustine (30 μM) causes G2/M arrest^[2]. Lomustine (CCNU) reduces the viability of F98 rat orthotopic glioma cells and Tu-2449 mouse glioma cell line, with IC₅₀s of 20.8 µM and 18.6 µM, respectively^[3].

In Vivo: Lomustine (CCNU) (30 mg/kg) in combination with Toca 511 + 5-FC prolongs survival in rats bearing F98 tumor cells. Lomustine (CCNU) (30 mg/kg) combined with Toca-511 + 5-FC also exhibits antitumor activity in the B6C3F1 mice bearing Tu-2449 glioma cells^[3].