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

Oxaliplatin Chemical Structure

CAS: 61825-94-3

规格 价格 库存 购买数量
50mg RMB 572.83 现货
200mg RMB 1704.66 现货
1g RMB 5487.3 现货
10g RMB 24488.1 现货
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客户使用Selleck的Oxaliplatin发表文献220

产品质控

批次: 纯度: 99.76%
99.76

Oxaliplatin相关产品

DNA/RNA Synthesis抑制剂选择性比较

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
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
DNA synthesis [1]
(RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, HT-144 cells)
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
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
NCT05068531 Recruiting
Colorectal Cancer Metastatic
Centre hospitalier de l''Université de Montréal (CHUM)|Exactis Innovation|Chaire Roger Des Groseillers d''oncologie chirurgicale HBP de l''Université de Montréal|Canexia Health
September 1 2022 --
NCT05031975 Recruiting
Colorectal Cancer
Fondazione IRCCS Istituto Nazionale dei Tumori Milano
May 2 2022 Phase 2
NCT05025826 Recruiting
Metastatic Gastric Cancer
Nantes University Hospital|Algosource
April 1 2022 Not Applicable

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
批次:

Water : 5 mg/mL

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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常见问题及建议解决方法

问题 1:
Is it ok to dissolve Oxaliplatin in saline?

回答:
Oxaliplatin is partially converted to cisplatin and L-isomers when dissolved in saline. The L-isomer of oxaliplatin is inactive. DMF is a better choice.

问题 2:
Is it ok to dissolve Oxaliplatin in DMSO?

回答:
Even though cis-platin is soluble in DMSO, the use of DMSO to dissolve cis– or trans-diamminedichloroplatinum (DDP) 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.

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