Oxaliplatin

製品コードS1224 バッチS122413

印刷

化学情報

 Chemical Structure 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 1.5 mg/mL warmed with 50ºC water bath (3.77 mM)
DMF 1.25 mg/mL (3.14 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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Oxaliplatin は autophagy を活性化する DNA alkylator です。Oxaliplatin は、RT4、TCCSUP、A2780、HT-29、U-373MG、U-87MG、SK-MEL-2、および HT-144 細胞において DNA 付加体を形成することにより、DNA/RNA Synthesis を阻害します。溶液は不安定なため、新鮮に調製する必要があります。DMSO は白金ベースの薬剤の溶解には推奨されません。薬剤の不活化を容易に招く可能性があります。
in vitro

The main mechanism of action of Oxaliplatin is mediated through the formation of DNA–adducts. This compound induces primary and secondary DNA lesions that lead to cell apoptosis. It is active against human melanoma cell lines C32 and G361 with IC50 of 0.98 mM and 0.14 mM, respectively. This chemical 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.

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. This compound (5mg/kg, i.v. on days 1, 5 and 9) is active on T-leukemia-lymphoma L40 AKR with T/C of 1.77. It is also efficient on intracerebrally grafted L1210 leukemia, MA 16-C xenografts, B16 melanoma xenografts, Lewis lung xenografts and C26 colon carcinoma xenografts. This chemical induces impairment of retrograde neuronal transport in mice.

特徴 This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).

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 this compound exposure. The plates are incubated at 37 °C in 5% CO2 and 100% relative humidity at all times except when adding this chemical 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

  • https://pubmed.ncbi.nlm.nih.gov/9834817/
  • https://pubmed.ncbi.nlm.nih.gov/11142694/
  • https://pubmed.ncbi.nlm.nih.gov/18043128/
  • https://pubmed.ncbi.nlm.nih.gov/8261411/
  • https://pubmed.ncbi.nlm.nih.gov/15619139/
  • https://pubmed.ncbi.nlm.nih.gov/19780708/
  • https://pubmed.ncbi.nlm.nih.gov/2675999/
  • https://pubmed.ncbi.nlm.nih.gov/23029238/
  • https://pubmed.ncbi.nlm.nih.gov/24812268/

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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人間や獣医の診断であるか治療的な使用のためにでない。

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