Phosphoramide mustard cyclohexanamine (2.1-20.7 mg/kg; i.p.; daily; for 5 days) inhibits subcutaneous tumor growth in rats. Phosphoramide mustard cyclohexanamine exhibits terminal elimination half-lives (rat 15.1 min) following intravenous administration (rat 59.4 mg/kg). Animal Model: Rat, subcutaneously implanted Walker 256 carcinosarcoma tumor Dosage: 2.1 mg/kg, 4.8 mg/kg, 10.4 mg/kg, 20.7 mg/kg Administration: Intraperitoneal injection, once daily, for 5 consecutive days Result: Required to produce 50% inhibition of subcutaneous tumor growth with dose of 12 mg/kg. Animal Model: Rats Dosage: 86.0 mg/kg (Pharmacokinetic Analysis) Administration: Intravenous injection Result: T 1/2 (15.1 min).

Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication. Phosphoramide mustard cyclohexanamine (3-6 μM; 48 hours) reduces cell viability in rat spontaneously immortalized granulosa cells (SIGCs). Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces DNA adduct formation and ovarian DNA damage. Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) increases DNA damage responses (DDR) gene mRNA expression levels and DDR proteins. Cell Viability Assay Cell Line: SIGCs Concentration: 0.5 μM, 1 μM, 3 μM, 6 μM Incubation Time: 48 hours Result: Reduced cell viability at concentrations of 3 μM and higher. RT-PCR Cell Line: SIGCs Concentration: 3 μM, 6 μM Incubation Time: 24 hours, 48 hours Result: Increased DDR gene mRNA expression levels. Western Blot Analysis Cell Line: SIGCs Concentration: 3 μM, 6 μM Incubation Time: 24 hours, 48 hours Result: Generally increased DDR proteins.

Phosphoramide mustard cyclohexanamine 是环磷酰胺 (HY-17420) 的活性代谢物，具有抗肿瘤活性。Phosphoramide mustard cyclohexanamine 能诱导 DNA 损伤