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磷酰胺氮芥

磷酰胺氮芥,10159-53-2,结构式
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
磷酰胺氮芥化学性质
  • 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)
安全信息
  • 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。
  • 靶点

    DNA Alkylator

  • 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).
磷酰胺氮芥上下游产品信息
上游原料
下游产品
磷酰胺氮芥生产厂家
  • 公司名称:TargetMol Chemicals Inc.
  • 联系电话:+1-781-999-5354 +1-00000000000
  • 电子邮件:marketing@targetmol.com
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  • 公司名称:TargetMol中国(陶术生物)
  • 联系电话: 4008200310
  • 电子邮件:marketing@tsbiochem.com
  • 国家:中国
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  • 公司名称:上海一飞生物科技有限公司
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  • 公司名称:河南天孚化工有限公司
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  • 电子邮件:info@tianfuchem.com
  • 国家:中国
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