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Oxaliplatin.

(Synonyms: 奥沙利铂)

目录号: PC10324 纯度: ≥98%

Oxaliplatin是一种DNA合成抑制剂。它会导致DNA交联损伤，阻止DNA复制和转录并导致细胞死亡。

CAS No. :61825-94-3

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中文名称	Oxaliplatin.
中文别名	奥沙利铂;左旋反式二氨环己烷草酸铂;己草铂;奥沙利铂(抗肿瘤医药中间体);(SP-4-2)-((1R,2R)-1,2-环己二胺-N,N')(乙二酸(2-)-O,O')铂;奥萨力铂;草酸铂;奥利沙铂;奥萨力铂,奥沙利铂;奥沙利铂对照;草酸铂 EP标准品;喷托维林;炔诺酮;(反-1,2-环己烷二胺)草酸铂(II);奥沙利铂对照品
英文名称	Eloxatin (TN)
英文别名	Oxaliplatin;L-OHP;[SP-4-2-(1R-TRANS)]-(1,2-CYCLOHEXANEDIAMINE-N,N')[ETHANEDIOATA(2-)-O,O']PLATINUM;trans-l-diaminocyclohexane oxalatoplatinum;(1,2-cyclohexanediamine-n,n’)(ethanedioato(2-)-o,o’)-platinu(sp-4-2-(1r-tr;1-ohp;oxalato(1r,2r-cyclohexanediammine)platinum(ii);oxalatoplatin;oxalatoplatinum;Oxaliplatin DMF;Dacplat;Elocatin;[SP-4-2-(1R-trans)]-(1,2-Cyclohexanediamine-N,N′)[ethanedioata(2--)-O,O’]platinum;(trans-1,2-Cyclohexanediamine)oxalatoplatinum(II);Eloxatin (TN);Oxaliplatin (JAN/USAN/INN);Oxaliplatin (Eloxatin);s1224;SW219151-1;O0372;D01790;AB01568250_01;15171-
Cas No.	61825-94-3
分子式	C₈H₁₄N₂O₄Pt
分子量	397.29
包装储存	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
详情描述	Oxaliplatin是一种DNA合成抑制剂。它会导致DNA交联损伤，阻止DNA复制和转录并导致细胞死亡。

生物活性

Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. Oxaliplatin can be used for cancer research.

性状

Solid

IC50 & Target[1][2]

IC50: DNA synthesis

体外研究(In Vitro)

Oxaliplatin (24-72 hours; 2-128 μM; HCC, HCCLM3 and Hep3B cells) inhibits cell growth and induces apoptosis.
Oxaliplatin (10 μM; 15-240 mins; CEM cells ) induces primary and secondary DNA lesions, including DNA cross-links (ISC) and DNA-protein cross-links (DPC).
Oxaliplatin (0.01 to 100 μM; 24 hours) potently inhibits 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	HCC, HCCLM3 and Hep3B cells
Concentration:	24, 48 and 72 hours
Incubation Time:	2, 4, 8, 16, 32, 64 and 128 μM
Result:	Decreased cell viability in a dose- and time-dependent manner.

Cell Cycle Analysis

Cell Line:	HCCLM3 and Hep3B cells
Concentration:	10 μM
Incubation Time:	24 hours
Result:	Increased the percentage of apoptotic cells (17.70% for HCCLM3 cells; 21.19% for Hep3B cells).

Cell Cycle Analysis

Cell Line:	HCCLM3 cells
Concentration:	10 μM
Incubation Time:	48 hours
Result:	Down-regulated the expression of Bcl-2 and Bcl-xL, and increased the expression of Bax.

体内研究(In Vivo)

Oxaliplatin (5-10 mg/kg; i.p.; for 32 days; nude mice) inhibits tumor growth.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice
Dosage:	5 and 10 mg/kg
Administration:	Intraperitoneal injection; for 32 days
Result:	Reduced tumor volume in HCCLM3 tumor xenografts.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

ClinicalTrial

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. [Information]

[2]. Mohammed MQ, et al. Oxaliplatin is active 体外研究 against human melanoma cell lines: comparison with NSC 119875 and NSC 241240. Anticancer Drugs. 2000 Nov;11(10):859-63. [Information]

[3]. Pendyala L, et al. 体外研究 cytotoxicity, protein binding, red blood cell partitioning, and biotransformation of oxaliplatin. Cancer Res. 1993 Dec 15;53(24):5970-6. [Information]

[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 [Information]

[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. [Information]

[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. [Information]

[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. [Information]

[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. [Information]

[9]. Garrett MJ, et, al. Capecitabine, Oxaliplatin, and Bevacizumab (BCapOx) Regimen for Metastatic Colorectal Cancer. Hosp Pharm. 2017 May;52(5):341-347. [Information]

溶解度数据

体外研究:

H₂O : 2.17 mg/mL (5.46 mM; ultrasonic and warming and heat to 60°C; DMSO can inactivate Oxaliplatins activity)

DMF : 1.67 mg/mL (4.20 mM; Need ultrasonic; DMSO can inactivate Oxaliplatins activity)

Ethanol : < 1 mg/mL (insoluble; DMSO can inactivate Oxaliplatins activity)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5171 mL	12.5853 mL	25.1705 mL
5 mM	0.5034 mL	2.5171 mL	5.0341 mL
10 mM	---	---	---

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 5% w/v Glucose Solution
Solubility: 3.33 mg/mL (8.38 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： PBS
Solubility: 1.92 mg/mL (4.83 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. Raymond E, et al. Oxaliplatin: a review of preclinical and clinical studies. Ann Oncol. 1998 Oct;9(10):1053-71. [Information]

[2]. Mohammed MQ, et al. Oxaliplatin is active 体外研究 against human melanoma cell lines: comparison with NSC 119875 and NSC 241240. Anticancer Drugs. 2000 Nov;11(10):859-63. [Information]

[3]. Pendyala L, et al. 体外研究 cytotoxicity, protein binding, red blood cell partitioning, and biotransformation of oxaliplatin. Cancer Res. 1993 Dec 15;53(24):5970-6. [Information]

[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 [Information]

[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. [Information]

[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. [Information]

[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. [Information]

[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. [Information]

[9]. Garrett MJ, et, al. Capecitabine, Oxaliplatin, and Bevacizumab (BCapOx) Regimen for Metastatic Colorectal Cancer. Hosp Pharm. 2017 May;52(5):341-347. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Oxaliplatin.

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