Oxaliplatin
- 貨號 Cat. No.
- S1224
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
Oxaliplatin
Oxaliplatin inhibits DNA synthesis by conforming DNA adducts.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Oxaliplatin inhibits DNA synthesis by conforming DNA adducts. | |||||
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| 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] | |||||
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Protocol(Only for Reference)
Cell Assay: [4]
| Cell lines | RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2 and HT-144 cell lines |
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| Concentrations | ~100 μM |
| Incubation Time | 48 hours |
| Method | 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 |
Animal Study: [6]
| Animal Models | Human hepatocellular carcinoma xenografts HCCLM3 |
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| Dosages | 10 mg/kg |
| Administration | A weekly i.p. injection |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01959139 | Not yet recruiting | Metastatic Pancreatic Adenocarcinoma | Southwest Oncology Group|National Cancer Institute (NCI)|Halozyme Therapeutics | 2013-12 | Phase 1|Phase 2 |
| NCT01928290 | Not yet recruiting | Stomach Neoplasms|Esophageal Neoplasms | Washington University School of Medicine | 2013-12 | Phase 2 |
| NCT01992705 | Not yet recruiting | Resectable Pancreatic Cancer | University of Maryland | 2014-01 | Phase 0 |
| NCT01675999 | Not yet recruiting | Colon Cancer|Locally Advanced Malignant Neoplasm | Assistance Publique - H么pitaux de Paris|Federation Francophone de Cancerologie Digestive|UNICANCER|Association de Recherche Experimentale et Clinique en Chirurgie Digestive|Association Europ茅enne de Recherche en Oncologie|Merck Serono S.A., Geneva | 2014-01 | Phase 2 |
| NCT02017704 | Not yet recruiting | Adenocarcinoma of the Prostate | Sidney Kimmel Comprehensive Cancer Center|Nucletron | 2014-02 | Phase 2 |
Chemical Information
| Molecular Weight (MW) | 397.29 |
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| Formula | C8H14N2O4Pt |
| CAS No. | 61825-94-3 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 14 mg/mL (35 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <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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Customer Reviews (2)
![]() Click to enlarge | Rating | |
| Source | Dr. Edita Aksamitiene from Thomas Jefferson University.Oxaliplatin purchased from Selleck | |
| Method | Cell viability assay | |
| Cell Lines | MiaPaca-2 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 72 h | |
| Results | Oxaliplatin potently inhibited the survival of MiaPaCa-2 cells in a dose-dependent manner. |
Product Citations (4)
A Novel Use of Gentamicin in the ROS-Mediated Sensitization of NCI- H460 Lung Cancer Cells to Various Anticancer Agents [Cuccarese MF ACS Chem Biol 2013;8(12):2771-7]
A novel use of gentamicin in the ROS-mediated sensitization of NCI-H460 lung cancer cells to various anticancer agents. [Cuccarese MF, et al. ACS Chem Biol 2013;8(12):2771-7]
Significance of mTOR signaling and its inhibitor against cancer stem-like cells in colorectal cancer. [Cai Z, et al. Ann Surg Oncol 2014;21(1):179-88]
