Phosphoramide mustard is a biologically active metabolite of Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard induces DNA damage.

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

Phosphoramide mustard (2.1-20.7 mg/kg; i.p.; daily; for 5 days) inhibits subcutaneous tumor growth in rats[2]. Phosphoramide mustard exhibits terminal elimination half-lives (rat 15.1 min) following intravenous administration (rat 59.4 mg/kg)[2]. Animal Model: Rat, subcutaneously implanted Walker 256 carcinosarcoma tumor[2]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[2]Dosage: 59.4 mg/kg (Pharmacokinetic Analysis) Administration: Intravenous injection Result: T 1/2 (15.1 min).

10159-53-2

C4H11Cl2N2O2P

221.02

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years