Phosphoramide mustard (cyclohexanamine)

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Phosphoramide mustard (cyclohexanamine)  纯度: ≥95.0%

Phosphoramide mustard cyclohexanamine 是环磷酰胺 (HY-17420) 的活性代谢物,具有抗肿瘤活性。Phosphoramide mustard cyclohexanamine 能诱导 DNA 损伤。

Phosphoramide mustard (cyclohexanamine)

Phosphoramide mustard (cyclohexanamine) Chemical Structure

CAS No. : 1566-15-0

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Phosphoramide mustard (cyclohexanamine) 相关产品

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生物活性

Phosphoramide mustard cyclohexanamine is a biologically active metabolite of Cyclophosphamide (HY-17420), with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA damage[1][2].

体外研究
(In Vitro)

Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication[1].
Phosphoramide mustard cyclohexanamine (3-6 μM; 48 hours) reduces cell viability in rat spontaneously immortalized granulosa cells (SIGCs)[1].
Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces DNA adduct formation and ovarian DNA damage[1].
Phosphoramide mustard cyclohexanamine (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 cyclohexanamine (2.1-20.7 mg/kg; i.p.; daily; for 5 days) inhibits subcutaneous tumor growth in rats[2].
Phosphoramide mustard cyclohexanamine 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: 86.0 mg/kg (Pharmacokinetic Analysis)
Administration: Intravenous injection
Result: T1/2 (15.1 min).

分子量

320.20

Formula

C10H24Cl2N3O2P

CAS 号

1566-15-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

H2O : 100 mg/mL (312.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1230 mL 15.6152 mL 31.2305 mL
5 mM 0.6246 mL 3.1230 mL 6.2461 mL
10 mM 0.3123 mL 1.5615 mL 3.1230 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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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