磷酰胺氮芥
- CAS号:10159-53-2
- 英文名:phosphoramide mustard
- 中文名:磷酰胺氮芥
- CBNumber:CB01386806
- 分子式:C4H11Cl2N2O2P
- 分子量:221.02
- MOL File:10159-53-2.mol
- 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)
- 毒性 :LD50 intraperitoneal in mouse: 184mg/kg
磷酰胺氮芥性质、用途与生产工艺
- 生物活性 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。
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靶点
DNA Alkylator
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体外研究
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. -
体内研究
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).
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