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Oxaliplatin

Oxaliplatin

产品编号 T0164   CAS 61825-94-3
别名: L-OHP, 奥沙利铂

Oxaliplatin (L-OHP) 是一种 DNA 烷化剂,一种 DNA 合成抑制剂。Oxaliplatin 会导致 DNA 交联损伤,阻止 DNA 复制和转录并导致细胞死亡。Oxaliplatin 可以诱导细胞自噬

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Oxaliplatin Chemical Structure
Oxaliplatin, CAS 61825-94-3
规格 价格/CNY 货期 数量
25 mg ¥ 268 现货
50 mg ¥ 460 现货
100 mg ¥ 686 现货
200 mg ¥ 1,178 现货
500 mg ¥ 1,750 现货
其他形式的 Oxaliplatin:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Oxaliplatin (T0164)
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纯度: 99.93%
纯度: 99.63%
纯度: 98.47%
纯度: 98%
纯度: 97%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.
体外活性 方法:人结肠癌细胞 HT29、SW620、WiDr 和 LS174T 用 Oxaliplatin (0.001 ng/ml-100 µg/mL) 处理 24 h,使用 MTT 方法检测细胞毒性。
结果:Oxaliplatin 对 HT29、SW620、WiDr 和 LS174T 细胞具有细胞毒性,IC50 分别为 0.33、1.13、0.13 和 0.19 μg/mL。[1]
方法:人结肠癌细胞 HCT116 WT 和 CHK2 KO 用 Oxaliplatin (40 µM) 处理 24-96 h,使用 Flow Cytometry 方法检测细胞凋亡情况。
结果:Oxaliplatin 处理 24-96 h,WT 和 CHK2-KO 细胞系中的凋亡水平增加。处理 24-72 h,WT 细胞的凋亡水平始终比 CHK2 KO 细胞低两倍。然而,处理 96 h,WT 和 CHK2-KO 细胞的凋亡水平相同 (85%)。[2]
方法:人口腔鳞状细胞癌细胞 CAL27 用 Oxaliplatin (31.25-125 μM)、SCC25 用 Oxaliplatin (25-100 μM) 处理 12-36 h,使用 Wound-healing 方法检测细胞迁移情况。
结果:Oxaliplatin 以剂量依赖的方式对 CAL27 和 SCC25 细胞的迁移具有抑制作用。[3]
体内活性 方法:为检测体内抗肿瘤活性,将 Oxaliplatin (5 mg/kg) 和 piperlongumine (2.5 mg/kg) 腹腔注射给携带人结直肠癌肿瘤 HCT-116 的 BALB/c nu/nu 小鼠,每天一次,持续二十四天。
结果:Oxaliplatin 和 piperlongumine 联合治理显著抑制肿瘤生长。Piperlongumine 可以通过 ROS 介导的细胞凋亡在体内使肿瘤对 Oxaliplatin 敏感。[4]
方法:为建立铂类药物诱导的疼痛性周围神经病变模型,将 Oxaliplatin (3 mg/kg/天) 腹腔注射给 C57BL6J 小鼠,注射五天,休息五天,持续两个周期。
结果:Oxaliplatin 治疗组的小鼠表现出显著的机械性异常性疼痛。Oxaliplatin 组在后足表现出明显的冷痛觉过敏。[5]
激酶实验 Binding experiments of electrophysiology: CHO cells expressing the subunit of the voltage-dependent L-type Ca2+ channel are cultrured in medium without serum in the presence of different concentrations of Nisoldipine. Then Ca2+ channel current elicited from a holding potential of -100 mV or -50 mV is recorded at room temperature with the whole-cell configuration of the patch-clamp method using the List EPC-7 patch-clamp amplifer and pClamp software. The concentration of competitor inhibiting 50% of the specific binding represents IC50.
细胞实验 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(Only for Reference)
别名 L-OHP, 奥沙利铂
化合物与蛋白结合的复合物

T0164_2

NMR Solution Structure of an Oxaliplatin 1,2-d(GG) Intrastrand Cross-Link in a DNA Dodecamer Duplex

分子量 397.29
分子式 C8H14N2O4Pt
CAS No. 61825-94-3

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble)

DMSO: 50 mg/mL (125.85 mM), DMSO inactivates the activity of Oxaliplatin.

H2O: 3 mg/mL (7.55 mM), Sonification and heating to 60℃ are recommended.

DMF: 1.67 mg/mL (4.20 mM), Sonification is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O / DMF 1 mM 2.5171 mL 12.5853 mL 25.1705 mL 62.9263 mL
DMSO / H2O 5 mM 0.5034 mL 2.5171 mL 5.0341 mL 12.5853 mL
DMSO 10 mM 0.2517 mL 1.2585 mL 2.5171 mL 6.2926 mL
20 mM 0.1259 mL 0.6293 mL 1.2585 mL 3.1463 mL
50 mM 0.0503 mL 0.2517 mL 0.5034 mL 1.2585 mL
100 mM 0.0252 mL 0.1259 mL 0.2517 mL 0.6293 mL

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TargetMol Library Books参考文献

1. Nannizzi S, et al. Cellular and molecular mechanisms for the synergistic cytotoxicity elicited by oxaliplatin and pemetrexed in colon cancer cell lines. Cancer Chemother Pharmacol. 2010 Aug;66(3):547-58. 2. Pires IM, et al. Oxaliplatin responses in colorectal cancer cells are modulated by CHK2 kinase inhibitors. Br J Pharmacol. 2010 Mar;159(6):1326-38. 3. Li D, et al. Oxaliplatin induces the PARP1-mediated parthanatos in oral squamous cell carcinoma by increasing production of ROS. Aging (Albany NY). 2021 Jan 20;13(3):4242-4257. 4. Chen W, et al. The synergistic effects of oxaliplatin and piperlongumine on colorectal cancer are mediated by oxidative stress. Cell Death Dis. 2019 Aug 8;10(8):600. 5. Ta LE, et al. Mice with cisplatin and oxaliplatin-induced painful neuropathy develop distinct early responses to thermal stimuli. Mol Pain. 2009 Feb 26;5:9. 6. Zhou Y, Yang L, Xiong L, et al. KIF11 is upregulated in colorectal cancer and silencing of it impairs tumor growth and sensitizes colorectal cancer cells to oxaliplatin via p53/GSK3β signaling[J]. Journal of Cancer. 2021, 12(12): 3741. 7. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 8. Yang P, Liu W, Fu R, et al. Cucurbitacin E Chemosensitizes Colorectal Cancer Cells via Mitigating TFAP4/Wnt/β-Catenin Signaling[J]. Journal of Agricultural and Food Chemistry. 2020 9. Wang X, Wu F, Wang H, et al. PDCD6 cooperates with C-Raf to facilitate colorectal cancer progression via Raf/MEK/ERK activation[J]. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-15. 10. Huang Y, Wang H, Hao Y, et al. Myeloid PTEN promotes chemotherapy-induced NLRP3-inflammasome activation and antitumour immunity[J]. Nature Cell Biology. 2020: 1-12.(22-6 , 716–727)

TargetMol Library Books文献引用

1. Chao S, Zhang F, Yan H, et al.Targeting intratumor heterogeneity suppresses colorectal cancer chemoresistance and metastasis.EMBO reports.2023: e56416. 2. Jiang Y, Feng Y, Huang J, et al.LAD1 promotes malignant progression by diminishing ubiquitin-dependent degradation of vimentin in gastric cancer.Journal of Translational Medicine.2023, 21(1): 1-15. 3. Feng Y, Cao Z, Xu A, et al.Evaluation of toxicity and mutagenicity of oxaliplatin on germ cells in an alternative in vivo model Caenorhabditis elegans.Food and Chemical Toxicology.2023: 113902. 4. Yu Y, Wu T, Zhang X, et al.Regorafenib activates oxidative stress by inhibiting SELENOS and potentiates oxaliplatin-induced cell death in colon cancer cells.European Journal of Pharmacology.2023: 175986. 5. Zhang Z, Ye J, Liu X, et al.Huangqi Guizhi Wuwu decoction alleviates oxaliplatin-induced peripheral neuropathy via the gut-peripheral nerve axis.Chinese Medicine.2023, 18(1): 1-15. 6. Feng W Q, Zhang Y C, Gao H, et al.FOXD1 promotes chemotherapy resistance by enhancing cell stemness in colorectal cancer through β‑catenin nuclear localization.Oncology Reports.2023, 50(1): 1-14. 7. Li J, Lv J, Chen Y, et al.Tumor suppressor circPDE4D inhibits the progression of colorectal cancer and regulates oxaliplatin chemoresistance.Gene.2023: 147323. 8. Zhao L, Liu S, Zhang X, et al.Satellite glial cell-secreted exosomes after in-vitro oxaliplatin treatment presents a pro-nociceptive effect for dorsal root ganglion neurons and induce mechanical hypersensitivity in naïve mice.Molecular and Cellular Neuroscience.2023: 103881. 9. Liu M, Mai J W, Luo D X, et al.NFATc2-dependent Epigenetic Downregulation of the TSC2/Beclin-1 Pathway is Involved in Neuropathic Pain Induced by Oxaliplatin.Molecular Pain.2023: 17448069231158289. 10. Glorieux C, Xia X, You X, et al. Cisplatin and gemcitabine exert opposite effects on immunotherapy with PD-1 antibody in K-ras-driven cancer. Journal of Advanced Research. 2021
11. Huang Y, Wang H, Hao Y, et al. Myeloid PTEN promotes chemotherapy-induced NLRP3-inflammasome activation and antitumour immunity. Nature Cell Biology. 2020: 1-12.(22-6 , 716–727) 12. Wang X, Wu F, Wang H, et al. PDCD6 cooperates with C-Raf to facilitate colorectal cancer progression via Raf/MEK/ERK activation. Journal of Experimental & Clinical Cancer Research. 2020, 39(1): 1-15 13. Zhou Y, Yang L, Xiong L, et al. KIF11 is upregulated in colorectal cancer and silencing of it impairs tumor growth and sensitizes colorectal cancer cells to oxaliplatin via p53/GSK3β signaling. Journal of Cancer. 2021, 12(12): 3741. 14. Lee E J, Yang J H, Choi J G, et al. Augmented Antitumor Effect of Unripe Rubus coreanus Miquel Combined with Oxaliplatin in a Humanized PD-1/PD-L1 Knock-In Colorectal Cancer Mouse Model. Cells. 2022, 11(18): 2876. 15. Lin W, Zou H, Mo J, et al. Micro1278 Leads to Tumor Growth Arrest, Enhanced Sensitivity to Oxaliplatin and Vitamin D and Inhibits Metastasis via KIF5B, CYP24A1, and BTG2, Respectively. Frontiers in Oncology. 2021 Mar 11;11:637878. doi: 10.3389/fonc.2021.637878. eCollection 2021. 16. Shen X, Zhang Y, Xu Z, et al. KLF5 inhibition overcomes oxaliplatin resistance in patient-derived colorectal cancer organoids by restoring apoptotic response. Cell Death & Disease. 2022, 13(4): 1-13 17. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation. Journal of chemical information and modeling. 2019, 59(10): 4374-4382. 18. Yang P, Liu W, Fu R, et al. Cucurbitacin E Chemosensitizes Colorectal Cancer Cells via Mitigating TFAP4/Wnt/β-Catenin Signaling. Journal of Agricultural and Food Chemistry. 2020 Nov 18. doi: 10.1021 19. Bi G, Liang J, Zhao M, et al. MiR-6077 promotes cisplatin/pemetrexed resistance in lung adenocarcinoma by targeting CDKN1A/cell cycle arrest and KEAP1/ferroptosis pathways. Molecular Therapy-Nucleic Acids. 2022 20. Qiao S, Lu W, Glorieux C, et al. Wild-type IDH2 protects nuclear DNA from oxidative damage and is a potential therapeutic target in colorectal cancer. Oncogene. 2021: 1-13. 21. Su C, Cheng C, Rong Z, et al.Repurposing fluphenazine as an autophagy modulator for treating liver cancer.Heliyon.2023 22. Lee E J, Kim Y S, Kim J H, et al.Uncovering the colorectal cancer immunotherapeutic potential: Evening primrose (Oenothera biennis) root extract and its active compound oenothein B targeting the PD-1/PD-L1 blockade.Phytomedicine.2024: 155370.
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该产品包含在如下化合物库中:
抗癌上市药物库 抑制剂库 抗癌药物库 酪氨酸激酶分子库 抗癌临床化合物库 药物功能重定位化合物库 抗癌活性化合物库 DNA 损伤和修复分子库 细胞周期化合物库 FDA 上市药物库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

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Keywords

Oxaliplatin 61825-94-3 Autophagy Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA Alkylator/Crosslinker DNA/RNA Synthesis L-OHP DNA cross-links anticancer 奥沙利铂 Inhibitor apoptosis inhibit inhibitor

 

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