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Oxaliplatin 目录号 GC17716

Antitumor agent

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50mg
¥347.00
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100mg
¥630.00
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200mg
¥1,082.00
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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Cell experiment [1,2]:

Cell lines

Carcinoma cell lines

Preparation method

Limited soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1-24h

Applications

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-373MG and U-87MG, and melanoma cell lines SK-MEL-2 and HT-144 with IC50 of 11 μM, 15 μM, 0.17 μM, 0.97 μM, 2.95 μM, 17.6 μM, 30.9 μM and 7.85 μM, respectively.Oxaliplatin was active against C32 and G361 cell lines with IC50 values of 49.48 and 9.07 μM (1 h), 9.47 and 1.30 μM (4 h), and 0.98 and 0.14 μM (24 h).

Animal experiment [3,4]:

Animal models

Nude mice bearing hepatocellular HCCLM3 tumors, Mice bearing L1210 leukemia, MA 16-C xenografts, B16 melanoma xenografts, Lewis lung xenografts and C26 colon carcinoma xenografts.

Dosage form

Intraperitoneal injection, 10 mg/kg, weekly injection; 5 mg/kg, Intravenous injection, on days 1, 5 and 9

Application

Oxaliplatin significantly reduced tumor volume and apoptotic index in nude mice bearing hepatocellular HCCLM3 tumors. 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.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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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Chemical Properties

Cas No. 61825-94-3 SDF
化学名 (1R,2R)-cyclohexane-1,2-diamine;oxalate;platinum(2+)
Canonical SMILES C1CCC(C(C1)N)N.C(=O)(C(=O)[O-])[O-].[Pt+2]
分子式 C8H14N2O4Pt 分子量 397.29
溶解度 ≥37.25mg/mL in DMSO, ≥3.94mg/mL in H2O with gentle warming 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

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.