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Lomustine

CAS No. : 13010-47-4

MCE 站：Lomustine

产品活性：Lomustine (CCNU; NSC 79037) 是一种 DNA 烷化剂 (DNA alkylator)，具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Autophagy  |  Apoptosis

作用靶点：DNA Alkylator/Crosslinker  |  Autophagy  |  Apoptosis

In Vitro: Lomustine (CCNU; NSC 79037) 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. 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. Lomustine (CCNU) reduces the viability of F98 rat orthotopic glioma cells and Tu-2449 mouse glioma cell line, with IC₅₀s of 20.8 ?M and 18.6 ?M, respectively.

In Vivo: Lomustine (CCNU; NSC 79037) (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.

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