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Cyclophosphamide
CAS No. : 50-18-0
MCE 国际站:Cyclophosphamide
产品活性:Cyclophosphamide 是一种合成的 DNA Alkylator,在化学上与氮芥类有关,具有抗肿瘤及免疫抑制活性。
作用靶点:DNA Alkylator/Crosslinker
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. Cyclophosphamide inhibits the AChE reversibly with an IC50 of 511 μM. Carbon tetrachloride does not affect the direct cytotoxicity of cyclophosphamide or 4-hydroxycyclophosphamide to cells in culture.
In Vivo: Cyclophosphamide can be used in animal modeling to establish bone marrow suppression model. 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.
Cyclophosphamide (CP) is a prodrug that is enzymatically converted to the cytotoxic 4-hydroxycyclophosphamide (4OHCP) by hepatic enzymes, the cytochrome P450. Cyclophosphamide has vast interspecies and intraspecies variations in kinetics. Dog microsomes were 55-fold more efficient than human microsomes, 2.8-fold more efficient than cat microsomes, and 1.2-fold more efficient than mouse microsomes at catalyzing CP bioactivation.
Administration: 150 mg/kg • ip • single dose.
Administration: 150 mg/kg • ip • single dose.
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