Phosphoramide mustard 是环磷酰胺 (HY-17420) 的活性代谢物,具有抗肿瘤活性。Phosphoramide mustard 能诱导 DNA 损伤。
生物活性 | Phosphoramide mustard is a biologically active metabolite of Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard induces DNA damage[1][2]. |
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体外研究 (In Vitro) | 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. |
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体内研究 (In Vivo) | 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: | T1/2(15.1 min). |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |