Cyclophosphamide

50-18-0

C7H15Cl2N2O2P

H2O : >= 55 mg/mL (210.66 mM); DMSO : >= 38 mg/mL (145.54 mM)

Cell Cycle/DNA Damage

Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities. IC50 & Target: DNA Alkylator^[1] In Vitro: Cyclophosphamide induces outer membrane blebbing, leads to DNA fragmentation, as revealed by TUNEL staining of free 3'-OH DNA ends, and induces cleavage of the caspase 3 and caspase 7 substrate PARP in 9L/P450 cells. Bcl-2 expression fully blocks the activation of both initiator caspases as well as the effector caspase 3 in cells treated with activated Cyclophosphamide. Bcl-2 inhibits the cytotoxic effects but not the cytostatic effects of activated Cyclophosphamide^[1]. Cyclophosphamide inhibits the AChE reversibly with an IC₅₀ of 511 uM^[2]. Carbon tetrachloride does not affect the direct cytotoxicity of cyclophosphamide or 4-hydroxycyclophosphamide to cells in culture^[3]. In Vivo: Cyclophosphamide (injected i.p.; 2mg/mouse in 0.1 mL PBS, in C3H mice bearing SW1 tumors) increases the percentage of cells that stained for CD3, CD4 or CD8 in both spleens and tumors^[4].