Oxaliplatin

製品コードS1224 バッチS122411

化学情報

	Synonyms	L-OHP,NSC 266046	Storage (From the date of receipt)	2 years 4°C(in the dark) powder
	化学式	C₈H₁₄N₂O₄Pt
	分子量	397.29	CAS No.	61825-94-3
Solubility (25°C)*	体外	Water	2 mg/mL warmed with 50ºC water bath (5.03 mM)
		Ethanol	Insoluble

* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
in vitro	The main mechanism of action of Oxaliplatin is mediated through the formation of DNA–adducts. Oxaliplatin induces primary and secondary DNA lesions that lead to cell apoptosis. ^[1] Oxaliplatin is active against human melanoma cell lines C32 and G361 with IC50 of 0.98 mM and 0.14 mM, respectively. ^[2] Oxaliplatin effectively 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. ^[4]
in vivo	A weekly i.p. injection of Oxaliplatin at 10 mg/kg to nude mice bearing hepatocellular HCCLM3 tumors significantly reduces tumor volume and apoptotic index. ^[6] Oxaliplatin (5mg/kg, i.v. on days 1, 5 and 9) is active on T-leukemia-lymphoma L40 AKR with T/C of 1.77. Oxaliplatin is also efficient on intracerebrally grafted L1210 leukemia, MA 16-C xenografts, B16 melanoma xenografts, Lewis lung xenografts and C₂₆ colon carcinoma xenografts. ^[7] Oxaliplatin induces impairment of retrograde neuronal transport in mice. ^[8]
特徴	This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).^[9]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2 and HT-144 cell lines
	濃度	~100 μM
	反応時間	48 hours
	実験の流れ	The cytotoxicity studies are carried out with the sulforhodamine-B microculture colorimetrie assay. Typically, cells are plated into 96-well plates on day 0 and exposed to Oxaliplatin on day 1; the sulforhodamine-B assay is carried out 48 h after Oxaliplatin exposure. The plates are incubated at 37 °C in 5% CO₂ and 100% relative humidity at all times except when adding Oxaliplatin and during the final assay period. The initial number of cells plated for the assay ranged from 2-20 × 10³ cells/50 /nL/well. The numbers of cells for plating and the drug exposure time are based on pilot studies using the criteria that (a) the cells in control wells are still in the log phase of growth on the day of the assay; (b) the maximum absorbance for the untreated controls on the day of the assay is in the range of 1.0 to 1.5; and (c) cells go through >2 doublings during the drug exposure. Eight wells are used per concentration. The plates are read at 570 and/or 540 nm using a Biotek Instruments model EL309 microplate reader interfaced with an IBM PC-compatible computer. The data are transferred and transformed into a LOTUS 1-2-3 format by the computer program DATALOG, and survival fractions are calculated by comparing the drug treated with control
動物実験	動物モデル	Human hepatocellular carcinoma xenografts HCCLM3
	投薬量	10 mg/kg
	投与方法	A weekly i.p. injection

参考

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カスタマーフィードバック

: Data from [J Proteomics, 2014, 10.1016/j.jprot.2014.10.009]

: Data from [Optical Methods for Tumor Treatment and Detection, 2013, 10.1117/12.2010730]

: , 2013, Dr. Edita Aksamitiene from Thomas Jefferson University

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