Oxaliplatin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Oxaliplatin主要通过顺应DNA加合物而抑制DNA合成。Oxaliplatin是一种铂化合物,具有广谱的抗肿瘤活性,与其它铂类化合物缺乏交叉抗性。Oxaliplatin诱导原发性和继发性DNA损伤,引发细胞凋亡。
体外实验:Oxaliplatin对人黑色素瘤细胞系C32和G361具有活性,IC50分别为0.98 mM和0.14 mM。Oxaliplatin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、成胶质细胞瘤细胞系U-373MG和U-87MG以及黑色素瘤细胞系SK-MEL-2和HT-144,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。
在体实验:在具有肝细胞HCCLM3肿瘤的裸鼠中,腹腔注射10 mg/kg oxaliplatin,每周一次,oxaliplatin显著减少肿瘤体积和凋亡指数。在第1、5和9天静脉内注射5 mg/kg的 oxaliplatin,对T淋巴瘤L40 AKR有活性,T/C为1.77。在脑内移植L1210白血病、MA16-C异种移植物、B16黑素瘤异种移植物、Lewis肺异种移植物和C26结肠癌异种移植物的模型中,Oxaliplatin具有有效的活性。Oxaliplatin损伤小鼠逆行神经元转运。在实验过程中,Cisplatin(3 mM)溶于盐水溶剂,Carboplatin(27 mM)和oxaliplatin(12.6 mM)溶于水中。
临床试验:在转移性结肠直肠癌患者中,Oxaliplatin与 fluorouracil/folinic acid联合使用对转移性结肠直肠具有活性,Oxaliplatin可以作为一线治疗方法并对以前化疗难以治愈患者产生治疗效果。此外,Oxaliplatin在铂进行预处理的卵巢癌、非霍奇金淋巴瘤、乳腺癌、间皮瘤和非小细胞肺癌的患者中具有功效。
参考文献:
[1]. Culy CR, Clemett D, Wiseman LR. Oxaliplatin. A review of its pharmacological properties and clinical efficacy in metastatic colorectal cancer and its potential in other malignancies. Drugs. 2000 Oct;60(4):895-924.
[2]. Raymond E, Faivre S, Chaney S et al. Cellular and molecular pharmacology of oxaliplatin. Mol Cancer Ther. 2002 Jan;1(3):227-35.
[3]. Stein A, Arnold D. Oxaliplatin: a review of approved uses. Expert Opin Pharmacother. 2012 Jan;13(1):125-37.
[4]. Hoff PM, Saad ED, Costa F et al. Literature review and practical aspects on the management of oxaliplatin-associated toxicity. Clin Colorectal Cancer. 2012 Jun;11(2):93-100.
[5]. Hall MD, et al. Say no to DMSO: dimethylsulfoxide inactivates cisplatin, carboplatin, and other platinum complexes. Cancer Res. 2014 Jul 15;74(14):3913-22.
- 1. Qing Zhang, Yue Zhou, et al. "Low-dose orlistat promotes the therapeutic effect of oxaliplatin in colorectal cancer." Biomed Pharmacother. 2022 Sep;153:113426. PMID: 36017794
- 2. Xia Liao, Yaoyao Zhang, et al. "Inositol hexaphosphate sensitizes hepatocellular carcinoma to oxaliplatin relating inhibition of CCN2-LRP6-β-catenin-ABCG1 signaling pathway." J Cancer. 2021 Aug 24;12(20):6071-6080. PMID: 34539880
- 3. Liao X, Song G, et al. "Oxaliplatin resistance is enhanced by saracatinib via upregulation Wnt-ABCG1 signaling in hepatocellular carcinoma." BMC Cancer. 2020;20(1):31. PMID: 31931755
- 4. Feng M, Jin JQ, et al. "Pharmacological inhibition of β-catenin/BCL9 interaction overcomes resistance to immune checkpoint blockades by modulating T(reg) cells." Sci Adv. 2019 May 8;5(5):eaau5240. PMID: 31086813
- 5. Cho SY, Chae J, et al. "Unstable Genome and Transcriptome Dynamics during Tumor Metastasis Contribute to Therapeutic Heterogeneity in Colorectal Cancers." Clin Cancer Res. 2019 Jan 22. PMID: 30670495
- 6. Goodspeed A, Jean A, et al. "A Whole-genome CRISPR Screen Identifies a Role of MSH2 in Cisplatin-mediated Cell Death in Muscle-invasive Bladder Cancer." Eur Urol. 2019 Feb;75(2):242-250. PMID: 30414698
- 7. Andrew Goodspeed, Annie Jean, et al. "Low MSH2 protein levels identify muscle-invasive bladder cancer resistant to cisplatin." bioRxiv. 2018 June 29.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 397.29 |
Cas No. | 61825-94-3 |
Formula | C8H14N2O4Pt |
Solubility | insoluble in EtOH; ≥37.25 mg/mL in DMSO; ≥3.94 mg/mL in H2O with gentle warming |
Chemical Name | (1R,2R)-cyclohexane-1,2-diamine;oxalate;platinum(2+) |
SDF | Download SDF |
Canonical SMILES | C1CCC(C(C1)N)N.C(=O)(C(=O)[O-])[O-].[Pt+2] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1,2]: | |
细胞系 |
癌细胞系 |
溶解方法 |
该化合物在DMSO中的溶解度有限。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
1-24h |
应用 |
Oxaliplatin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、黑素瘤细胞系SK-MEL-2和HT-144,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。Oxaliplatin对C32和G361细胞系有活性,IC50值分别为49.48和9.07 μM(1h)、9.47和1.30 μM(4h)、0.98和0.14 μM(24h)。 |
动物实验 [3,4]: | |
动物模型 |
携带肝细胞HCCLM3肿瘤的裸鼠,携带L1210白血病的小鼠,MA 16-C异种移植裸鼠,B16黑色素瘤异种移植裸鼠,Lewis肺和C26结肠癌异种移植裸鼠。 |
给药剂量 |
腹腔注射,10 mg/kg,每周注射;5 mg/kg,静脉注射,第1、5和9天 |
应用 |
Oxaliplatin显著降低携带肝细胞HCCLM3肿瘤裸鼠的肿瘤体积和凋亡指数。Oxaliplatin(5 mg/kg,第1、5和9天静脉注射)对T-白血病-淋巴瘤L40 AKR有活性,T/C为1.77。Oxaliplatin对于颅内移植的L1210白血病、B16黑色素瘤异种移植物、MA16-C异种移植物、Lewis肺异种移植物和C26结肠癌异种移植物有效。Oxaliplatin诱导小鼠逆行神经元运输的损伤。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Mohammed M Q, Retsas S. Oxaliplatin is active in vitro against human melanoma cell lines: comparison with cisplatin and carboplatin[J]. Anti-cancer drugs, 2000, 11(10): 859-863. [2]. Pendyala L, Creaven P J. In vitro cytotoxicity, protein binding, red blood cell partitioning, and biotransformation of oxaliplatin[J]. Cancer research, 1993, 53(24): 5970-5976. [3]. Wang Z, Zhou J, Fan J, et al. Oxaliplatin induces apoptosis in hepatocellular carcinoma cells and inhibits tumor growth[J]. Expert opinion on investigational drugs, 2009, 18(11): 1595-1604. [4]. Mathe G, Kidani Y, Segiguchi M, et al. Oxalato-platinum or 1-OHP, a third-generation platinum complex: an experimental and clinical appraisal and preliminary comparison with cis-platinum and carboplatinum[J]. Biomedicine & pharmacotherapy, 1989, 43(4): 237-250. |
质量控制和MSDS
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