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！

目录号：S1224 Purity: 99.76%

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

规格	价格	库存
50mg	572.83	现货
200mg	1704.66	现货
1g	5487.3	现货
10g	24488.1	现货
更大包装有超大折扣
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产品质控

批次：纯度： 99.76%

99.76

Oxaliplatin相关产品

相关靶点	tRNA synthetase RdRp DNA synthesis helicase ribonucleotide reductase	点击展开
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相关化合物库	FDA药物库天然产物库凋亡分子化合物库 DNA损伤/ DNA修复化合物库细胞周期化合物库	点击展开

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

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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
[1] Raymond E et al, Ann Oncol, 1998, 9(10), 1053-1071. [2] Mohammed MQ, et al. Anticancer Drugs, 2000, 11(10), 859-863. [3] Kirstein MN, et al. Anticancer Drugs, 2008, 19(1), 37-44. [4] Pendyala L, et al. Cancer Res, 1993, 53(24), 5970-5976. [5] Espinosa M, et al. Cancer Chemother Pharmacol, 2005, 55(3), 301-305. [6] Wang Z, et al. Expert Opin Investig Drugs, 2009, 18(11), 1595-1604. [7] Math?G, et al. Biomed Pharmacother, 1989, 43(4), 237-250. [8] Schellingerhout D, et al. PLoS One, 2012, 7(9), e45776. [9] Matthew D Hall, et al. Cancer Res. 2014 Jul 15;74(14):3913-22. + 展开

参考文献

+ 展开

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 (12.58 mM)

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
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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。

技术支持

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操作手册

如果有其他问题，请给我们留言。

* 必填项

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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):