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Oxaliplatin

现货
Catalog No.
A8648
抗肿瘤剂
组合的产品项目
规格价格库存 数量
50mg
¥ 500.00
现货
100mg
¥ 850.00
现货
200mg
¥ 1,450.00
现货

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Background

Oxaliplatin inhibits DNA synthesis, primarily by conforming DNA adducts. Oxaliplatin, a platinum compound, has a broad spectrum of anti-tumor activity and has demonstrated a lack of cross-resistance with other platinum compounds. Oxaliplatin induces primary and secondary DNA lesions that lead to cell apoptosis.

In vitro: Oxaliplatin is active against human melanoma cell lines C32 and G361 with the IC50 values of 0.98 mM and 0.14 mM, respectively. Oxaliplatin effectively inhibited bladder carcinoma cell lines RT4 and TCCSUP, ovarian carcinoma cell line A2780, colon carcinoma cell line HT-29, glioblastoma cell lines U-87MG and U-373MG, and melanoma cell lines SK-MEL-2 and HT-144 with the IC50 values of 11 μM, 15 μM, 0.17 μM, 0.97 μM, 17.6 μM, 2.95 μM, 30.9 μM and 7.85 μM, respectively.

In vivo: A weekly injection of Oxaliplatin (10 mg/kg, i.p.) to nude mice bearing hepatocellular HCCLM3 tumors significantly reduces tumor volume and apoptotic index. Oxaliplatin (5 mg/kg, i.v. on days 1, 5 and 9) was active on T-leukemia-lymphoma L40 AKR with T/C of 1.77. Oxaliplatin was also efficient on intracerebrally grafted L1210 leukemia, B16 melanoma xenografts, MA 16-C xenografts, Lewis lung xenografts and C26 colon carcinoma xenografts. Oxaliplatin induced impairment of retrograde neuronal transport in mice.

Clinical Trials: In patients with metastatic colorectal cancer, in combination with fluorouracil/folinic acid, Oxaliplatin showed its activity against metastatic colorectal, both as a first-line therapy and in patients refractory to previous chemotherapy. In addition, oxaliplatin has also shown efficacy in patients with platinum-pretreated ovarian cancer, non-Hodgkin's lymphoma, breast cancer, mesothelioma and non-small cell lung cancer.

References:
[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.

文献引用

1. 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
2. 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
3. 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
4. Andrew Goodspeed, Annie Jean, et al. "Low MSH2 protein levels identify muscle-invasive bladder cancer resistant to cisplatin." bioRxiv. 2018 June 29.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt397.29
Cas No.61825-94-3
FormulaC8H14N2O4Pt
Solubility≥37.25mg/mL in DMSO, ≥3.94mg/mL in H2O with gentle warming
Chemical Name(1R,2R)-cyclohexane-1,2-diamine;oxalate;platinum(2+)
SDFDownload SDF
Canonical SMILESC1CCC(C(C1)N)N.C(=O)(C(=O)[O-])[O-].[Pt+2]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

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.

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Oxaliplatin

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Oxaliplatin

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