Oxaliplatin inhibits DNA synthesis by conforming DNA adducts.

Oxaliplatin有效作用于脑内移植的L1210白血病,MA 16-C移植瘤,B16黑色素瘤移植瘤,Lewis肺癌移植瘤和C26 结肠癌移植瘤.对携带肝癌HCCLM3肿瘤的裸鼠每周腹腔注射10 mg/kg Oxaliplatin,可以明显降低肿瘤体积和凋亡指数.Oxaliplatin作用于小鼠,诱导退行性神经转导降低.

Oxaliplatin有效抑制膀胱癌细胞系RT4和TCCSUP,卵巢癌细胞系A2780,结肠癌细胞系HT-29,胶质母细胞瘤细胞系U-373 mg和U-87 mg和黑色素瘤细胞株SK-MEL-2和HT-144（IC50分别为11 μM, 15 μM, 0.17 μM, 0.97 μM, 2.95 μM, 17.6 μM, 30.9 μM 和 7.85 μM）。Oxaliplatin还能有效抑制人类黑色素瘤细胞系C32和G361（IC50分别为0.98 mM 和0.14 mM）。

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.

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)

61825-94-3

C8H14N2O4Pt

397.294

奥沙利铂;L-OHP;Oxaliplatin

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[1]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） [2]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. [3]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. [4]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 [5]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. [6]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 [7]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 [8]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. [9]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 [10]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.

DMSO:20 mg/mL(50.3 mM),DMSO can inactivate Oxaliplatin's activity
H2O:3 mg/mL (7.55 mM),ultrasonic and warming and heat to 60°C
Ethanol:< 1 mg/mL (insoluble)
DMF:1.67 mg/mL (4.20 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years