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。
| 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].
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. |
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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].
| 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). |
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| 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 | 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℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 100 mg/mL (312.30 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
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