磷酰胺氮芥
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- CAS号:
- 10159-53-2
- 英文名:
- phosphoramide mustard
- 英文别名:
- phosphoramide mustard;Phosphoramide Mustard D8
- 中文名:
- 磷酰胺氮芥
- 中文别名:
- 磷酰胺氮芥
- CBNumber:
- CB01386806
- 分子式:
- C4H11Cl2N2O2P
- 分子量:
- 221.02
- MOL File:
- 10159-53-2.mol
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磷酰胺氮芥化学性质
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熔点:
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115 °C
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沸点:
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363.5±52.0 °C(Predicted)
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密度:
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1.474±0.06 g/cm3(Predicted)
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酸度系数(pKa):
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0.41±0.50(Predicted)
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磷酰胺氮芥性质、用途与生产工艺
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。
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
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Cell Line:
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SIGCs
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Concentration:
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0.5 μM, 1 μM, 3 μM, 6 μM
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Incubation Time:
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48 hours
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Result:
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Reduced cell viability at concentrations of 3 μM and higher.
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RT-PCR
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Cell Line:
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SIGCs
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Concentration:
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3 μM, 6 μM
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Incubation Time:
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24 hours, 48 hours
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Result:
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Increased DDR gene mRNA expression levels.
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Western Blot Analysis
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Cell Line:
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SIGCs
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Concentration:
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3 μM, 6 μM
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Incubation Time:
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24 hours, 48 hours
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Result:
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Generally increased DDR proteins.
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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).
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Animal Model:
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Rat, subcutaneously implanted Walker 256 carcinosarcoma tumor
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Dosage:
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2.1 mg/kg, 4.8 mg/kg, 10.4 mg/kg, 20.7 mg/kg
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Administration:
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Intraperitoneal injection, once daily, for 5 consecutive days
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Result:
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Required to produce 50% inhibition of subcutaneous tumor growth with dose of 12 mg/kg.
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Animal Model:
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Rats
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Dosage:
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59.4 mg/kg (Pharmacokinetic Analysis)
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Administration:
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Intravenous injection
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Result:
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T
1/2
(15.1 min).
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磷酰胺氮芥
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10159-53-2, 磷酰胺氮芥 相关搜索:
- 磷酰胺氮芥
- 10159-53-2
- Phosphoramide Mustard D8
- phosphoramide mustard