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^[1]

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.