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国际站：Oxaliplatin
中文名：奥沙利铂
CAS：61825-94-3
品牌：MedChemExpress (MCE)
存储条件：4°C, protect from light
生物活性：Oxaliplatin 是一种DNA 合成 抑制剂。 Oxaliplatin 引起 DNA 交联损伤，阻止 DNA 复制和转录并诱导细胞凋亡。奥沙利铂可用于癌症研究[1][2][3]。 IC50 和目标：IC50：DNA 合成
体外：Oxaliplatin（24-72 小时；2-128 μM；HCC、HCCLM3 和 Hep3B 细胞）抑制细胞生长并诱导细胞凋亡[1]。
Oxaliplatin（10 μM；15-240 分钟； CEM 细胞 ) 诱导原发性和继发性 DNA 损伤，包括 DNA 交联 (ISC) 和 DNA-蛋白质交联 (DPC)[2]。
奥沙利铂（0.01 至 100 μM； 24 小时）有效抑制膀胱癌细胞系 RT4 和 TCCSUP、卵巢癌细胞系 A2780、结肠癌细胞系 HT-29、胶质母细胞瘤细胞系 U-373MG 和 U-87MG，以及黑色素瘤细胞系 SK-MEL-2 和 HT- 144 的 IC50 分别为 11 μM、15 μM、0.17 μM、0.97 μM、2.95 μM、17.6 μM、30.9 μM 和 7.85 μM[3]。
体内：奥沙利铂（5-10 mg/kg；腹腔注射；32 天；裸鼠）抑制肿瘤生长[1]。
参考文献：
[1]. Raymond E, et al. Oxaliplatin: a review of preclinical and clinical studies. Ann Oncol. 1998 Oct;9(10):1053-71.
[2]. Mohammed MQ, et al. Oxaliplatin is active in vitro against human melanoma cell lines: comparison with NSC 119875 and NSC 241240. Anticancer Drugs. 2000 Nov;11(10):859-63.
[3]. Pendyala L, et al. In vitro cytotoxicity, protein binding, red blood cell partitioning, and biotransformation of oxaliplatin. Cancer Res. 1993 Dec 15;53(24):5970-6.
[4]. Wang Z, et al. Oxaliplatin induces apoptosis in hepatocellular carcinoma cells and inhibits tumor growth. Expert Opin Investig Drugs. 2009 Nov;18(11):1595-604
[5]. Mathé G, et al. Oxalato-platinum or 1-OHP, a third-generation platinum complex: an experimental and clinical appraisal and preliminary comparison with cis-platinum. Biomed Pharmacother. 1989;43(4):237-50.
[6]. Schellingerhout D, et al. Impairment of retrograde neuronal transport in oxaliplatin-induced neuropathy demonstrated by molecular imaging. PLoS One. 2012;7(9):e45776. doi: 10.1371/journal.pone.0045776. Epub 2012 Sep 20.
[7]. Park GY, et al. Phenanthriplatin, a monofunctional DNA-binding platinum anticancer drug candidate with unusual potency and cellular activity profile. Proc Natl Acad Sci U S A. 2012 Jul 24;109(30):11987-92.
[8]. Yi Yao, et al. Comparative proteomic analysis of colon cancer cells in response to oxaliplatin treatment. Biochim Biophys Acta. 2009 Oct;1794(10):1433-40.
[9]. Garrett MJ, et, al. Capecitabine, Oxaliplatin, and Bevacizumab (BCapOx) Regimen for metastatic Colorectal Cancer. Hosp Pharm. 2017 May;52(5):341-347.
