产品说明书

Oxaliplatin

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Chemical Structure| 61825-94-3 同义名 : Lipoxal;RP 54780;SR96669.;Code names: JM83;LOHP;Abbreviations: 1OHP;Eloxatine;Dacplat;US brand name: Eloxatin Foreign brand names: Dacotin;oxalatoplatinum;oxalatoplatin;diaminocyclohexane oxalatoplatinum;NSC 266046
CAS号 : 61825-94-3
货号 : A100048
分子式 : C8H14N2O4Pt
纯度 : 98%
分子量 : 397.286
MDL号 : MFCD00866327
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 2 mg/mL(5.03 mM)，配合低频超声，并水浴加热至45℃助溶

DMF: 1.5 mg/mL(3.78 mM)，配合低频超声助溶
动物实验配方：

IP 2% DMSO+water 1 mg/mL clear

PO 0.5% CMC-Na 55 mg/mL suspension

生物活性
靶点

  • DNA synthesis
描述 DNA damage is an abnormal chemical structure in DNA, while a mutation is a change in the sequence of standard base pairs. Oxaliplatin is an alkylating agent that inhibits DNA synthesis and replication by generating DNA damage[1]. Oxaliplatin can induces immunogenic cell death by provoking the presentation of damage associated molecular patterns. Oxaliplatin inhibited human colorectal tumor cell lines HCT-8, HT-29 and HCT 116 with IC50 values of 0.87 μM, 0.88 μM and 0.53 μM, respectively[2]. Oxaliplatin inhibited human bladder cancer cell lines TCC SUP and RT-4 with IC50 values of 15.04 and 11.10 μM, respectively. Oxaliplatin inhibited human Glioma cell lines U-87MG and U-373MG with IC50 values of 17.60 and 2.95 μM, respectively[3]. Furthermore, oxaliplatin could active mTOR pathway via increasing the level of phosphorylated p70 S6 kinase in five ATCC cell lines HCT15, DLD-1, LoVo, HCT116, HT29 and Colo 205[4]. In vivo, administration of 10 mg/kg Oxaliplatin via tail vein injection once a week for 4 weeks significantly inhibited the MHCC97 cells subcutaneously tumor[5]. Treatment with Oxaliplatin at the dose of 10 mg/kg once a week for 4 weeks inhibited the growth of human hepatocellular HCCLM3 xenografts in nude mice[6]. Treatment with oxaliplatin at the dose of 10 mg/kg induced mTOR activation and immunogenic cell death in colon cancer xenografts model. In early clinical, oxaliplatin demonstrated clinical activity in a variety of tumors, including CRC, breast, endometrial cancers and malignant melanoma[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
A549 Growth Inhibition Assay IC50=5.8 ± 0.6 μM 25625243
A549 Growth Inhibition Assay IC50=51.08 ± 10.96 μM 25307448
A549/CDDP Growth Inhibition Assay IC50=18.6 ± 1.2 μM 25625243
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01157052 Neoplasms, Colorectal ... 展开 >> Colorectal Cancer Colorectal Carcinoma 收起 << Phase 1 Unknown September 2015 Canada, Alberta ... 展开 >> Cross Cancer Institute Not yet recruiting Edmonton, Alberta, Canada, T6G 1Z2 Sub-Investigator: Judith Meza-Junco, MD 收起 <<
NCT00005856 Adult Giant Cell Glioblastoma ... 展开 >> Adult Glioblastoma Adult Gliosarcoma 收起 << Phase 1 Phase 2 Terminated(Administratively co... 展开 >>mplete.) 收起 << - United States, Maryland ... 展开 >> New Approaches to Brain Tumor Therapy Consortium Baltimore, Maryland, United States, 21231-1000 收起 <<
NCT01795027 Gastric Cancer Phase 3 Unknown June 2018 China, Guangdong ... 展开 >> the central hospital of Chaozhou Chaozhou, Guangdong, China the 1st people's hospital of Foshan Foshan, Guangdong, China cancer center of Guangzhou medical college Guangzhou, Guangdong, China cancer center of Sun yat-sen University Guangzhou, Guangdong, China Guangdong Traditional Medical Hospital Guangzhou, Guangdong, China the 1st affliated hospital of Guangdong pharmacuetic college Guangzhou, Guangdong, China the 1St Affliated Hospital of Guangzhou Medical College Guangzhou, Guangdong, China the 6th affliated hospital of Sun-yat-sen University Guangzhou, Guangdong, China the 1st hospital of Shantou University Shantou, Guangdong, China the cental hospital of Shantou Shantou, Guangdong, China YUE-BEI people's hospital Shaoguan, Guangdong, China the 2nd people's hospital of Shenzhen Shenzhen, Guangdong, China the 5th hospital of Sun-yat-sen University Zhuhai, Guangdong, China 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.59mL

2.52mL

1.26mL

25.17mL

5.03mL

2.52mL
参考文献

[1]Arango D, Wilson AJ, Shi Q, Corner GA, Arañes MJ, Nicholas C, Lesser M, Mariadason JM, Augenlicht LH. Molecular mechanisms of action and prediction of response to oxaliplatin in colorectal cancer cells. Br J Cancer. 2004 Nov 29;91(11):1931-46. doi: 10.1038/sj.bjc.6602215. PMID: 15545975; PMCID: PMC2409767.

[2]Balin-Gauthier D, Delord JP, Rochaix P, Mallard V, Thomas F, Hennebelle I, Bugat R, Canal P, Allal C. In vivo and in vitro antitumor activity of oxaliplatin in combination with cetuximab in human colorectal tumor cell lines expressing different level of EGFR. Cancer Chemother Pharmacol. 2006 Jun;57(6):709-18. doi: 10.1007/s00280-005-0123-3. Epub 2005 Dec 1. PMID: 16320055.

[3]Rixe O, Ortuzar W, Alvarez M, Parker R, Reed E, Paull K, Fojo T. Oxaliplatin, tetraplatin, cisplatin, and carboplatin: spectrum of activity in drug-resistant cell lines and in the cell lines of the National Cancer Institute's Anticancer Drug Screen panel. Biochem Pharmacol. 1996 Dec 24;52(12):1855-65. doi: 10.1016/s0006-2952(97)81490-6. PMID: 8951344.

[4]Lu M, Zessin AS, Glover W, Hsu DS. Activation of the mTOR Pathway by Oxaliplatin in the Treatment of Colorectal Cancer Liver Metastasis. PLoS One. 2017 Jan 6;12(1):e0169439. doi: 10.1371/journal.pone.0169439. PMID: 28060954; PMCID: PMC5218497.

[5]Bu Y, Jia QA, Ren ZG, Zhang JB, Jiang XM, Liang L, Xue TC, Zhang QB, Wang YH, Zhang L, Xie XY, Tang ZY. Maintenance of stemness in oxaliplatin-resistant hepatocellular carcinoma is associated with increased autocrine of IGF1. PLoS One. 2014 Mar 14;9(3):e89686. doi: 10.1371/journal.pone.0089686. PMID: 24632571; PMCID: PMC3954560.

[6]Wang Z, Zhou J, Fan J, Qiu SJ, Yu Y, Huang XW, Sun J, Tan CJ, Dai Z. Oxaliplatin induces apoptosis in hepatocellular carcinoma cells and inhibits tumor growth. Expert Opin Investig Drugs. 2009 Nov;18(11):1595-604. doi: 10.1517/13543780903292626. PMID: 19780708.

[7]Misset JL, Bleiberg H, Sutherland W, Bekradda M, Cvitkovic E. Oxaliplatin clinical activity: a review. Crit Rev Oncol Hematol. 2000 Aug;35(2):75-93. doi: 10.1016/s1040-8428(00)00070-6. PMID: 10936465.