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Oxaliplatin
别名: L-OHP,NSC 266046 中文名称：奥沙利铂
铂类药物不建议使用DMSO溶解，易失活！
Oxaliplatin是一种DNA烷基化药物可以激活自噬。Oxaliplatin在RT4，TCCSUP，A2780，HT-29，U-373MG，U-87MG，SK-MEL-2，和 HT-144细胞中通过形成DNA加合物而抑制DNA合成。在溶液中不稳定，请现配现用！铂类药物不建议用DMSO溶解，易失活！
Oxaliplatin Chemical Structure
CAS: 61825-94-3
产品质控
批次：
纯度：
99.76%
99.76
Oxaliplatin相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| SW620 | Function Assay | 10 µg/ml | 24 h | increases LC3-II accumulation and decreases P62 expression | 25749420 |
| SW480 | Function Assay | 10 µg/ml | 24 h | increases LC3-II accumulation and decreases P62 expression | 25749420 |
| SW620 | Function Assay | 10 µg/ml | 24 h | enhances cellular autophagic flux | 25749420 |
| SW480 | Function Assay | 10 µg/ml | 24 h | enhances cellular autophagic flux | 25749420 |
| Panc-1 | Cell Viability Assay | 25/50 μM | 24/48 h | inhibits proliferation of PC cells in a synergistic manner combined with WA | 25444914 |
| MIAPaCa-2 | Cell Viability Assay | 25/50 μM | 24/48 h | inhibits proliferation of PC cells in a synergistic manner combined with WA | 25444914 |
| SW1990 | Cell Viability Assay | 25/50 μM | 24/48 h | inhibits proliferation of PC cells in a synergistic manner combined with WA | 25444914 |
| HPDE | Cell Viability Assay | 25/50 μM | 24/48 h | inhibits proliferation of PC cells in a synergistic manner combined with WA | 25444914 |
| Panc-1 | Apoptosis Assay | 25 µM | 24 h | induces apoptosis in a synergistic manner combined with WA | 25444914 |
| MIAPaCa-2 | Apoptosis Assay | 25 µM | 24 h | induces apoptosis in a synergistic manner combined with WA | 25444914 |
| Panc-1 | Function Assay | 25 µM | 24/48 h | induces cleavage of PARP, caspase-9, caspase-8 and caspase-3 | 25444914 |
| MIAPaCa-2 | Function Assay | 25 µM | 24/48 h | induces cleavage of PARP, caspase-9, caspase-8 and caspase-3 | 25444914 |
| SW480 | Growth Inhibition Assay | 1 μM | 0-72 h | inhibits cell growth in a time dependent manner | 24997451 |
| HT-29 | Growth Inhibition Assay | 1 μM | 0-72 h | inhibits cell growth in a time dependent manner | 24997451 |
| HCT116 | Function Assay | 2/5 µM | 24/48 h | suppresses survivin mRNA expression | 24761411 |
| SW620 | Growth Inhibition Assay | 10-70 mg/L | 24/48/72 h | inhibits cell growth in both time and dose dependent manner | 24646305 |
| Caco2 | Function Assay | 30 μM | 24 h | induces the expression of HO-1, AKR1C, and NQO1 | 24556415 |
| Caco2 | Function Assay | 3/10/30 μM | 16 h | increases the mRNA levels of AKR1C1, NQO1, HO-1, MRP2, andMRP3 dose-dependently | 24556415 |
| Caco2 | Function Assay | 30/100 μM | 16 h | activates Nrf2 | 24556415 |
| CT26 | Cell Viability Assay | 4 mM | 48 h | decreases cell viability to 53.2% | 26137012 |
| CT26 | Function Assay | 4 mM | 48 h | increases the expression levels of autophagy-related proteins, such as LC3-II, Beclin1 and ATG5 | 26137012 |
| CT26 | Function Assay | 4 mM | 48 h | induces autophagy | 26137012 |
| SK-OV-3 | Function Assay | 50 μM | 48 h | promotes sensitivity of ovarian carcinoma to NK cell-mediated cytolysis | 26138671 |
| OVCAR-5 | Function Assay | 20 μM | 24h | promotes sensitivity of ovarian carcinoma to NK cell-mediated cytolysis | 26138671 |
| PA-1 | Function Assay | 10 μM | 24h | promotes sensitivity of ovarian carcinoma to NK cell-mediated cytolysis | 26138671 |
| SK-OV-3 | Function Assay | 50 μM | 96 h | up-regulates the stress ligands for NK cell-activating receptors and TRAIL receptors | 26138671 |
| OVCAR-5 | Function Assay | 30 μM | 48h | up-regulates the stress ligands for NK cell-activating receptors and TRAIL receptors | 26138671 |
| PA-1 | Function Assay | 10 μM | 48h | up-regulates the stress ligands for NK cell-activating receptors and TRAIL receptors | 26138671 |
| SK-OV-3 | Function Assay | 50 μM | 96 h | triggeres the production of type I IFNs and chemokines | 26138671 |
| OVCAR-5 | Function Assay | 30 μM | 48h | triggeres the production of type I IFNs and chemokines | 26138671 |
| PA-1 | Function Assay | 10 μM | 24h | triggeres the production of type I IFNs and chemokines | 26138671 |
| SK-OV-3 | Cell Viability Assay | 0-100 μM | 24/48/72 h | inhibits cell viability in both time and dose dependent manner | 26138671 |
| OVCAR-5 | Cell Viability Assay | 0-60 μM | 24/48/72 h | inhibits cell viability in both time and dose dependent manner | 26138671 |
| PA-1 | Cell Viability Assay | 0-20 μM | 24/48 h | inhibits cell viability in both time and dose dependent manner | 26138671 |
| LoVo | Function Assay | 1/5 μM | 24/48 h | induces transcriptional repression of DUT-N | 26208523 |
| HCT116 p53+/+ | Function Assay | 1/5 μM | 24/48 h | induces transcriptional repression of DUT-N | 26208523 |
| CaES-17 | Cytotoxicity Assay | 0–160 μM | 48 h | IC50=5.5 ± 0.2 μM | 26474693 |
| HKESC-2 | Cytotoxicity Assay | 0–160 μM | 48 h | IC50=5.8 ± 0.5 μM | 26474693 |
| SW480 | Growth Inhibition Assay | 72 h | IC50=10.7±2.26 µg/mL | 25360631 | |
| HCT116 | Growth Inhibition Assay | 72 h | IC50=6.23±0.75 µg/mL | 25360631 | |
| SW480 | Growth Inhibition Assay | 48 h | IC50=20.8 ug/mL | 24720675 | |
| LoVo | Growth Inhibition Assay | 48 h | IC50=94.83 μM | 26269759 | |
| HCT116 | Growth Inhibition Assay | 48 h | IC50=11.86 μM | 26269759 | |
| SW480 | Growth Inhibition Assay | 48 h | IC50=1.87 μM | 26269759 | |
| HT29 | Growth Inhibition Assay | IC50=63 μM ± 18 | 26004084 | ||
| DLD-1 | Growth Inhibition Assay | IC50=32.2 μM | 26003085 | ||
| HT-29 | Growth Inhibition Assay | IC50=35.6 μM | 26003085 | ||
| SiHa | Growth Inhibition Assay | IC50=0.8 ± 0.1 μM | 25801007 | ||
| S3 | Growth Inhibition Assay | IC50=53.5 ± 1.5 μM | 25801007 | ||
| AGS | Growth Inhibition Assay | IC50=10.6 μM | 25789057 | ||
| MKN-45 | Growth Inhibition Assay | IC50=14.0 μM | 25789057 | ||
| TMK-1 | Growth Inhibition Assay | IC50=22.6 μM | 25789057 | ||
| SCM-1 | Growth Inhibition Assay | IC50=17.5 μM | 25789057 | ||
| HCT-15 | Growth Inhibition Assay | IC50=8.64 μM | 25761479 | ||
| DiFi | Growth Inhibition Assay | IC50=10.95 μM | 25761479 | ||
| DLD-1 | Growth Inhibition Assay | IC50=8.65 μM | 25761479 | ||
| COLO-320DM | Growth Inhibition Assay | IC50=5.38 μM | 25761479 | ||
| SNU-175 | Growth Inhibition Assay | IC50=1.51 μM | 25761479 | ||
| HT-29 | Growth Inhibition Assay | IC50=5.22 μM | 25761479 | ||
| A549 | Growth Inhibition Assay | IC50=5.8 ± 0.6 μM | 25625243 | ||
| A549/CDDP | Growth Inhibition Assay | IC50=18.6 ± 1.2 μM | 25625243 | ||
| COC1 | Growth Inhibition Assay | IC50=46.20 ± 3.14 μM | 25307448 | ||
| SGC7901 | Growth Inhibition Assay | IC50=21.73 ± 3.08 μM | 25307448 | ||
| A549 | Growth Inhibition Assay | IC50=51.08 ± 10.96 μM | 25307448 | ||
| HepG2 | Growth Inhibition Assay | IC50=14.24 ± 1.82 μM | 25307448 | ||
| MCF-7 | Growth Inhibition Assay | IC50=14.24 ± 1.82 μM | 25307448 | ||
| HCT-116 | Growth Inhibition Assay | IC50=6.24 ± 2.97 μM | 25307448 | ||
| HT-29 | Growth Inhibition Assay | IC50>50 μM | 25307448 | ||
| HEK293 | Growth Inhibition Assay | IC50=8.82 ± 5.59 μM | 25307448 | ||
| HUVEC | Growth Inhibition Assay | IC50=11.30 ± 1.02 μM | 25307448 | ||
| MC38 | Growth Inhibition Assay | IC50=23 μM ± 2 | 26004084 | ||
| SW620 | Growth Inhibition Assay | IC50=3.68 μM | 26023085 | ||
| SW480 | Growth Inhibition Assay | IC50=2.86 μM | 26023085 | ||
| RKO | Growth Inhibition Assay | IC50=1.23 μM | 26023085 | ||
| LoVo | Growth Inhibition Assay | IC50=1.2 μM | 26023085 | ||
| KM12 | Growth Inhibition Assay | IC50=4.37 μM | 26023085 | ||
| HCT116p53- | Growth Inhibition Assay | IC50=1.08 μM | 26023085 | ||
| HCT116 | Growth Inhibition Assay | IC50=1.04 μM | 26023085 | ||
| HCT15 | Growth Inhibition Assay | IC50=1.43 μM | 26023085 | ||
| HT29 | Growth Inhibition Assay | IC50=2.69 μM | 26023085 | ||
| DLD1 | Growth Inhibition Assay | IC50=2.01 μM | 26023085 | ||
| Colo205 | Growth Inhibition Assay | IC50=3.33 μM | 26023085 | ||
| BE | Growth Inhibition Assay | IC50=3.33 μM | 26023085 | ||
| HCT116 | Growth Inhibition Assay | IC50=0.41 ± 0.02 μM | 26148596 | ||
| HT29 | Growth Inhibition Assay | IC50=0.88 ± 0.2 μM | 26148596 | ||
| SNU-387 | Growth Inhibition Assay | IC50=25 ± 2.7 μM | 26160429 | ||
| SNU-475 | Growth Inhibition Assay | IC50＞30 μM | 26160429 | ||
| Hep-G2 | Growth Inhibition Assay | IC50=13.1 ± 1.6 μM | 26160429 | ||
| SNU-398 | Growth Inhibition Assay | IC50=6.5 ± 1.1 μM | 26160429 | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=23.1 ± 0.1 μM | 26211591 | ||
| MCF-7 | Growth Inhibition Assay | IC50=15.4 ± 0.3 μM | 26211591 | ||
| SK-BR-3 | Growth Inhibition Assay | IC50=31.0 ± 0.1 μM | 26211591 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Oxaliplatin是一种DNA烷基化药物可以激活自噬。Oxaliplatin在RT4，TCCSUP，A2780，HT-29，U-373MG，U-87MG，SK-MEL-2，和 HT-144细胞中通过形成DNA加合物而抑制DNA合成。在溶液中不稳定，请现配现用！铂类药物不建议用DMSO溶解，易失活！ | |
|---|---|---|
| 特性 | 不建议使用DMSO溶解。[9] | |
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Oxaliplatin 主要作用机制是形成DNA交联剂而发挥作用。Oxaliplatin 诱导DNA一级和二级结构损伤而导致细胞凋亡。[1] Oxaliplatin 有效作用于人类黑色素瘤细胞系C32 和G361，IC50分别为0.98 mM 和0.14 mM。[2] 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-373MG和U-87MG，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。[4] |
|||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2 和 HT-144 细胞系 | ||
| 浓度 | ~100 μM | |||
| 孵育时间 | 48 小时 | |||
| 方法 | 使用 sulforhodamine-B 显微培养比色测定法进行细胞毒性研究。实验第0天细胞接种在96孔板上，实验第1天使用Oxaliplatin 处理细胞，48小时后，进行sulforhodamine-B 检测。除了添加Oxaliplatin和最终实验测定期间，实验全程在37°C 下含5% CO2 和 100% 相对湿度的环境下进行。检测到细胞的初始数目为每孔2-20 × 103个细胞/50 nL。接种和药物处理期间细胞数目如下（a）检测时对照组细胞仍处于对数期生长;（b）检测时未处理的对照组细胞最大吸光度为1.0〜1.5；（c）用药物处理期间细胞经过2倍以上倍增。每种浓度放置8孔。使用Biotek仪器EL309酶标仪与IBM PC-兼容型计算机在570 和/或 540 nm处测定。通过计算机程序DATALOG将实验数据传输且转化为LOTUS 1-2-3格式，通过比较实验组和对照组计算存活分数。 |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | VEGFR-1 / NRP-1 p-AKT(Ser473) / AKT / PTEN / p-Src(Tyr416) p-Src(Y418) / p-FAK(Y861) |
|
18790786 | |
| Immunofluorescence | E-cadherin / Vimentin ATXN2L / G3BP1 |
|
30787271 | |
| Growth inhibition assay | Cell viability |
|
28339092 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Oxaliplatin按10 mg/kg 剂量每周腹腔注射给药携带肝癌HCCLM3肿瘤的裸鼠，显著降低肿瘤体积和凋亡指数。[6] Oxaliplatin 按5mg/kg剂量在实验第1, 5 和 9天静脉注射给药，有效作用于T型白血病淋巴瘤L40 AKR,T/C为1.77。Oxaliplatin也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。[7]Oxaliplatin作用于小鼠，诱导退行性神经转导降低。[8] |
|
|---|---|---|
| 动物实验 | Animal Models | 携带人类肝癌移植瘤HCCLM3的小鼠 |
| Dosages | 10 mg/kg | |
| Administration | 每周腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06320301 | Recruiting | Biliary Tract Cancer|Gemox Chemotherapy |
Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University|Suzhou Suncadia Biopharmaceuticals Co. Ltd. |
April 1 2024 | Phase 2 |
| NCT05922358 | Not yet recruiting | Gastrointestinal Tumors |
Fujian Cancer Hospital |
September 1 2023 | Phase 2 |
| NCT05780684 | Recruiting | Colorectal Cancer|Esophagus Cancer|Appendix Cancer|Small Bowel Cancer|Ampullary Cancer |
Dartmouth-Hitchcock Medical Center |
July 14 2023 | Not Applicable |
| NCT05322590 | Recruiting | Metastatic Colorectal Carcinoma|Neuropathy |
Bexion Pharmaceuticals Inc.|ICON plc|CTI Clinical Trial and Consulting Services |
January 9 2023 | Phase 1|Phase 2 |
|
化学信息&溶解度
| 分子量 | 397.29 | 分子式 | C8H14N2O4Pt |
| CAS号 | 61825-94-3 | SDF | Download Oxaliplatin SDF |
| Smiles | C1CCC(C(C1)[NH-])[NH-].C(=O)(C(=O)O)O.[Pt+2] | ||
| 储存条件(自收到货起) | 2年 4°C（避光） 粉末 | 此产品性质不稳定，需现配现用!建议您购买分装规格，或者在收到货后进行分装。 | |
|
体外溶解度 |
Water : 5 mg/mL (12.58 mM) Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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* 必填项
常见问题及建议解决方法
问题 1:
Is it ok to dissolve it in saline?
回答：
When dissolved in saline, it is partially converted to cisplatin and L-isomers. The L-isomer of this compound is inactive. DMF is a better choice.
问题 2:
Is it ok to dissolve it in DMSO?
回答：
Even though it is soluble in DMSO, the use of DMSO to dissolve this compound in biological studies is strongly discouraged. The DMSO inserts itself into the ligand and inactivates platin-containing compounds. DMF is a much better choice than DMSO.
