Phosphoramide mustard(Synonyms: 磷酰胺氮芥)

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Phosphoramide mustard (Synonyms: 磷酰胺氮芥)

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(Synonyms: 磷酰胺氮芥)

Phosphoramide mustard Chemical Structure

CAS No. : 10159-53-2

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Phosphoramide mustard 的其他形式现货产品:

Phosphoramide mustard (cyclohexanamine)

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].

IC50 & Target

DNA Alkylator[1]

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

分子量

221.02

Formula

C4H11Cl2N2O2P

CAS 号

10159-53-2

中文名称

磷酰胺氮芥

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.

参考文献
  • [1]. Shanthi Ganesan, et al. Phosphoramide mustard exposure induces DNA adduct formation and the DNA damage repair response in rat ovarian granulosa cells. Toxicol Appl Pharmacol. 2015 Feb 1; 282(3): 252–258.

    [2]. S Genka, et al. Brain and plasma pharmacokinetics and anticancer activities of cyclophosphamide and phosphoramide mustard in the rat. Cancer Chemother Pharmacol. 1990;27(1):1-7.

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