磷酰胺氮芥
磷酰胺氮芥 性质
| 熔点 | 115 °C |
|---|---|
| 沸点 | 363.5±52.0 °C(Predicted) |
| 密度 | 1.474±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 0.41±0.50(Predicted) |
磷酰胺氮芥 用途与合成方法
DNA Alkylator
Phosphoramide mustard causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication.
Phosphoramide mustard (3-6 μM; 48 hours) reduces cell viability in rat spontaneously immortalized granulosa cells (SIGCs).
Phosphoramide mustard (3-6 μM; 24-48 hours) induces DNA adduct formation and ovarian DNA damage.
Phosphoramide mustard (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 (2.1-20.7 mg/kg; i.p.; daily; for 5 days) inhibits subcutaneous tumor growth in rats.
Phosphoramide mustard 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: | 59.4 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Intravenous injection |
| Result: | T 1/2 (15.1 min). |
