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10159-53-2

中文名稱(chēng) 磷酰胺氮芥
英文名稱(chēng) phosphoramide mustard
CAS 10159-53-2
分子式 C4H11Cl2N2O2P
分子量 221.02
MOL 文件 10159-53-2.mol
10159-53-2 結(jié)構(gòu)式 10159-53-2 結(jié)構(gòu)式

基本信息

中文別名
磷酰胺氮芥
英文別名
phosphoramide mustard

物理化學(xué)性質(zhì)

熔點(diǎn)115 °C
沸點(diǎn)363.5±52.0 °C(Predicted)
密度1.474±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)0.41±0.50(Predicted)

安全數(shù)據(jù)

毒性LD50 intraperitoneal in mouse: 184mg/kg

常見(jiàn)問(wèn)題列表

生物活性
Phosphoramide mustard 是環(huán)磷酰胺 (HY-17420) 的活性代謝物,具有抗腫瘤活性。Phosphoramide mustard 能誘導(dǎo) DNA 損傷。
靶點(diǎn)

DNA Alkylator

體外研究

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.
體內(nèi)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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