Amifostine (hydrate)是一种广谱的正常细胞保护剂，主要用于减轻化疗或放疗对正常组织的毒性。
Cas No.:112901-68-5
Sample solution is provided at 25 µL, 10mM.
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Amifostine (hydrate) is a broad-spectrum cytoprotective agent primarily used to reduce the toxicity of chemotherapy or radiotherapy on normal tissues[1-2]. Amifostine is a prodrug that is metabolized in vivo by alkaline phosphatase into the active thiol metabolite WR-1065. WR-1065 scavenges free radicals generated by cisplatin or radiation, promotes DNA repair, thereby reducing the toxicity of chemotherapeutic agents on the kidneys, bone marrow, and nerves, and alleviating xerostomia induced by radiotherapy[3-4].
In vitro, pretreatment of murine myeloid progenitor 32D cells with Amifostine (100μg/mL) for 18 hours, followed by culture under growth factor deprivation conditions, Amifostine significantly inhibited cell apoptosis and attenuated caspase-3 activity. Amifostine promoted the nuclear translocation of NF-κB/Rel by reducing cytoplasmic IκBα levels[5]. In H9c2 cardiomyocytes, pretreatment with Amifostine (25-100μM) for 30 minutes, followed by incubation with Tert-butyl hydroperoxide (TBHP; 100μM) for 12 hours, Amifostine significantly reduced cell apoptosis and oxidative stress[6].
In vivo, intraperitoneal injection of Amifostine (200mg/kg) in bleomycin (3U/kg)-induced pulmonary fibrosis C57BL6/J mice (administered on days 1, 3, and 5 post-modeling), Amifostine significantly alleviated pulmonary inflammation and fibrosis, improved mitochondrial function, and restored cellular metabolic balance via the NAD⁺/SIRT1/AMPK pathway[7]. Subcutaneous injection of Amifostine (25mg/kg) in Oxaliplatin-induced peripheral sensory neuropathy Swiss albino mice (administered 30 minutes before each Oxaliplatin injection, twice a week for nine times), Amifostine significantly prevented mechanical hyperalgesia and cold allodynia, and reduced the expression of c-Fos, nitrotyrosine, and ATF3 in the dorsal root ganglia[8].
References:
[1] Capizzi RL, Scheffler BJ, Schein PS. Amifostine-mediated protection of normal bone marrow from cytotoxic chemotherapy. Cancer. 1993 Dec 1;72(11 Suppl):3495-501.
[2] Koukourakis MI. Amifostine in clinical oncology: current use and future applications. Anticancer Drugs. 2002 Mar;13(3):181-209.
[3] Kouvaris JR, Kouloulias VE, Vlahos LJ. Amifostine: the first selective-target and broad-spectrum radioprotector. Oncologist. 2007 Jun;12(6):738-47.
[4] Singh VK, Seed TM. The efficacy and safety of amifostine for the acute radiation syndrome. Expert Opin Drug Saf. 2019 Nov;18(11):1077-1090.
[5] Romano MF, Lamberti A, Bisogni R, et al. Amifostine inhibits hematopoietic progenitor cell apoptosis by activating NF-kappaB/Rel transcription factors. Blood. 1999 Dec 15;94(12):4060-6.
[6] Wu SZ, Tao LY, Wang JN, et al. Amifostine Pretreatment Attenuates Myocardial Ischemia/Reperfusion Injury by Inhibiting Apoptosis and Oxidative Stress. Oxid Med Cell Longev. 2017;2017:4130824.
[7] Guo F, Xu F, Li S, et al. Amifostine ameliorates bleomycin-induced murine pulmonary fibrosis via NAD+/SIRT1/AMPK pathway-mediated effects on mitochondrial function and cellular metabolism. Eur J Med Res. 2024 Jan 20;29(1):68.
[8] Pereira AF, Lino JA, Alves BWF, et al. Amifostine protects from the peripheral sensory neuropathy induced by oxaliplatin in mice. Braz J Med Biol Res. 2020 Sep 18;53(11):e10263.
Amifostine (hydrate)是一种广谱的正常细胞保护剂，主要用于减轻化疗或放疗对正常组织的毒性[1-2]。Amifostine是一种前体药物，在体内经碱性磷酸酶代谢为活性硫醇代谢物WR-1065。该代谢物能清除顺铂或放疗产生的自由基，促进DNA修复，从而降低化疗药物对肾脏、骨髓、神经的毒性，并减少放疗引起的口腔干燥[3-4]。
在体外，Amifostine（100μg/mL）预处理鼠源骨髓祖细胞32D细胞18小时，随后在生长因子剥夺条件下培养细胞，Amifostine显著抑制细胞凋亡并减弱caspase‑3活性，同时通过降低胞质IκBα水平促进NF‑κB/Rel核转位[5]。Amifostine（25-100μM）H9c2心肌细胞30分钟，随后使用Tert-butyl hydroperoxide （TBHP；100μM）孵育12小时，Amifostine显著减轻细胞凋亡和氧化应激[6]。
在体内，Amifostine（200mg/kg）腹腔注射处理博来霉素（3U/kg）诱导的肺纤维化C57BL6/J小鼠（在造模后第1、3、5天给药），Amifostine显著减轻肺部炎症和纤维化，改善线粒体功能，并通过NAD+/SIRT1/AMPK通路恢复细胞代谢平衡[7]。Amifostine（25mg/kg）皮下注射处理奥沙利铂诱导的外周感觉神经病变Swiss albino小鼠（在每次奥沙利铂注射前30分钟给药，每周两次，共九次），Amifostine显著预防机械性痛觉过敏和冷触觉异常，并减少背根神经节中c-Fos、硝基酪氨酸和ATF3的表达[8]。
| Cell experiment [1]: | |
Cell lines | H9c2 cardiomyocytes (rat cardiac cell line) |
Preparation Method | H9c2 cells were maintained in high-glucose Dulbecco’s Modified Eagle Medium (DMEM) supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were pretreated with Amifostine (25–100μM) for 30 minutes before exposure to tert-butyl hydroperoxide (TBHP; 100μM) for 12 hours to simulate oxidative stress. |
Reaction Conditions | 25–100μM; 30min pretreatment |
Applications | Amifostine pretreatment significantly attenuated TBHP-induced cell death and apoptosis, accompanied by reduced reactive oxygen species (ROS) production and preservation of mitochondrial membrane potential (ΔΨm). |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice were intratracheally instilled with Bleomycin (3U/kg) to induce pulmonary fibrosis. Amifostine (200mg/kg) was administered intraperitoneally on days 1, 3, and 5 post-bleomycin challenge. Lung tissues and bronchoalveolar lavage fluid (BALF) were collected on days 7 and 21 for analysis. |
Dosage form | 200mg/kg; i.p.; Three doses. |
Applications | Amifostine significantly attenuated bleomycin-induced pulmonary fibrosis, reduced lung inflammation (e.g., decreased inflammatory cells and cytokines in BALF), and improved survival rates. Amifostine also suppressed fibrosis markers (collagen, fibronectin, α-SMA) in lung tissues. |
References: | |
| Cas No. | 112901-68-5 | SDF | |
| 别名 | 氨磷汀三水合物,WR2721 trihydrate | ||
| Canonical SMILES | NCCCNCCSP(O)(O)=O.O.O.O | ||
| 分子式 | C5H15N2O3PS•3H2O | 分子量 | 268.3 |
| 溶解度 | PBS (pH 7.2): 5 mg/ml | 储存条件 | Store at 2-8°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 | 3.7272 mL | 18.6359 mL | 37.2717 mL |
| 5 mM | 745.4 μL | 3.7272 mL | 7.4543 mL |
| 10 mM | 372.7 μL | 1.8636 mL | 3.7272 mL |
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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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