Amifostine
(Synonyms: 氨磷汀; WR2721) 目录号 : GC15473
Amifostine是一种有机硫代磷酸盐，属于选择性广谱正常组织细胞保护剂。
Cas No.:20537-88-6
Sample solution is provided at 25 µL, 10mM.
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Amifostine, an inorganic thiophosphate, is a selective broad-spectrum cytoprotector of normal tissues[1]. Amifostine is dephosphorylated by alkaline phosphatase in the body to form the active metabolite WR-1065, which scavenges oxygen free radicals and enhances the DNA repair process [2]. Amifostine has been widely used to reduce the severity of acute oral mucositis caused by radiation[3].
In vitro, Amifostine treatment for 5 days significantly inhibited the proliferation of myelodysplastic syndrome (MDS) cells, with an IC50 value of 14μM[4]. Treatment with 100μg/ml Amifostine for 12 hours inhibited apoptosis of 32D cells and enhanced the nuclear level of NF-κB/Rel[5]. Amifostine treatment for 12 days at a concentration of 1mM significantly inhibited the proliferation of Dami cells, caused changes in cell morphology[6].
In vivo, Amifostine treatment at a single dose of 200mg/kg for 18h attenuated lipopolysaccharide (LPS)-induced lung vascular leak and inhibited neutrophil accumulation in the lung parenchyma within mice[7]. A single subcutaneous injection of Amifostine (200mg/kg) for 30 minutes later significantly induced the expression of HIF1α in the tissues of normal rats[8].
References:
[1] Koukourakis M I. Amifostine in clinical oncology: current use and future applications[J]. Anti-cancer drugs, 2002, 13(3): 181-209.
[2] Van den Berg J H, Beijnen J H, Balm A J M, et al. Future opportunities in preventing cisplatin induced ototoxicity[J]. Cancer treatment reviews, 2006, 32(5): 390-397.
[3] Kalman N S, Zhao S S, Anscher M S, et al. Current status of targeted radioprotection and radiation injury mitigation and treatment agents: a critical review of the literature[J]. International Journal of Radiation Oncology* Biology* Physics, 2017, 98(3): 662-682.
[4] Ribizzi I, Darnowski J W, Goulette F A, et al. Amifostine cytotoxicity and induction of apoptosis in a human myelodysplastic cell line[J]. Leukemia research, 2000, 24(6): 519-525.
[5] Romano M F, Lamberti A, Bisogni R, et al. Amifostine inhibits hematopoietic progenitor cell apoptosis by activating NF-κB/Rel transcription factors[J]. Blood, The Journal of the American Society of Hematology, 1999, 94(12): 4060-4066.
[6] Wang H, Yang B, Hu B, et al. The effect of amifostine on differentiation of the human megakaryoblastic Dami cell line[J]. Cancer Medicine, 2016, 5(8): 2012-2021.
[7] Fu P, Birukova A A, Xing J, et al. Amifostine reduces lung vascular permeability via suppression of inflammatory signalling[J]. European Respiratory Journal, 2009, 33(3): 612-624.
[8] Koukourakis M I, Giatromanolaki A, Chong W, et al. Amifostine induces anaerobic metabolism and hypoxia-inducible factor 1α[J]. Cancer chemotherapy and pharmacology, 2004, 53(1): 8-14.
Amifostine是一种有机硫代磷酸盐，属于选择性广谱正常组织细胞保护剂[1]。Amifostine在体内经碱性磷酸酶去磷酸化后形成活性代谢物WR-1065，可清除氧自由基并增强DNA修复过程[2]。Amifostine已广泛应用于减轻放射治疗引起的急性口腔黏膜炎严重程度[3]。
在体外，Amifostine处理5天能显著抑制骨髓增生异常综合征(MDS)细胞增殖，IC50值为14μM[4]。使用100μg/ml的Amifostine处理32D细胞12小时，可抑制细胞凋亡并提高细胞核内NF-κB/Rel水平[5]。当浓度为1mM时，Amifostine处理12天能显著抑制Dami细胞增殖并引起细胞形态改变[6]。
在体内，单次注射200mg/kg剂量的Amifostine 18小时后，可减轻脂多糖(LPS)诱导的小鼠肺血管渗漏，并抑制肺实质中性粒细胞聚集[7]。单次皮下注射200mg/kg剂量的Amifostine 30分钟，能显著诱导正常大鼠组织中HIF1α的表达[8]。
| Cell experiment [1]: | |
Cell lines | Dami cells |
Preparation Method | The Dami cells were cultured in RPMI 1640 medium containing 10% heat-inactivated fetal bovine serum (FBS) and 100U/ml of double antibiotics, under conditions of 37°C, 5% CO2 and 100% humidity for cultivation. Dami cells were inoculated into 6-well plates with a density of 5×105 cells/ml. The cells were subcultured every 2 days. The concentration of Amifostine in the culture medium was 0.01, 0.1, 1, and 5mM. The cell count and cell morphology were analyzed every two days, and the entire experiment lasted for 12 days. |
Reaction Conditions | 0.01, 0.1, 1, and 5mM; 12 days |
Applications | Amifostine treatment at a concentration higher than 1mM significantly inhibited the proliferation of Dami cells, caused changes in cell morphology. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Preparation Method | Adult male, 8-10-week old C57BL/6J mice, with an average weight of 20-25g, were anaesthetised with an intraperitoneal injection of ketamine (75mg/kg) and acepromazine (1.5mg/kg). LPS (0.7mg/kg) or sterile water was injected intratracheally in a small volume (20-30ml) using a 20-gauge catheter. Although water is a hypotonic solvent, it did not induce any noticeable injury in control animals injected with 20ml sterile water, when compared with untreated mice or mice injected with 20ml of normotonic physiological solution (data not shown). Mice were randomized to concurrently receive sterile saline solution or Amifostine (200mg/kg) by intraperitoneal injection to yield the experimental groups: (1) control; (2) LPS (0.7mg/kg) only; (3) Amifostine (200mg/kg) only; and (4) LPS (0.7mg/kg)+Amifostine (200mg/kg). After 18 hours, the lung tissues of the mice were collected for analysis. |
Dosage form | 200mg/kg for once; 18h; i.p. |
Applications | Amifostine treatment attenuated LPS-induced lung vascular leak and inhibited neutrophil accumulation in the lung parenchyma within mice. |
References: | |
| Cas No. | 20537-88-6 | SDF | |
| 别名 | 氨磷汀; WR2721 | ||
| 化学名 | S-(2-((3-aminopropyl)amino)ethyl) O,O-dihydrogen phosphorothioate | ||
| Canonical SMILES | NCCCNCCSP(O)(O)=O | ||
| 分子式 | C5H15N2O3PS | 分子量 | 214.22 |
| 溶解度 | ≥ 8.05mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.6681 mL | 23.3405 mL | 46.681 mL |
| 5 mM | 933.6 μL | 4.6681 mL | 9.3362 mL |
| 10 mM | 466.8 μL | 2.334 mL | 4.6681 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
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2.
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- Purity: >98.00%
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