Oxaliplatin

別名:L-OHP,NSC 266046

Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.

Oxaliplatin化学構造

CAS No. 61825-94-3

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 41500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)
JPY 595500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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Oxaliplatin関連製品

DNA/RNA Synthesis阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
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生物活性

製品説明 Oxaliplatin is a DNA alkylating agent that activates autophagy. Oxaliplatin inhibits DNA synthesis by conforming DNA adducts in RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, and HT-144 cells.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
特性 This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).[9]
Targets
DNA synthesis [1]
(RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, HT-144 cells)
In Vitro
In vitro

The main mechanism of action of Oxaliplatin is mediated through the formation of DNA–adducts. Oxaliplatin induces primary and secondary DNA lesions that lead to cell apoptosis. [1] Oxaliplatin is active against human melanoma cell lines C32 and G361 with IC50 of 0.98 mM and 0.14 mM, respectively. [2] Oxaliplatin effectively inhibits bladder carcinoma cell lines RT4 and TCCSUP, ovarian carcinoma cell line A2780, colon carcinoma cell line HT-29, glioblastoma cell lines U-373MG and U-87MG, and melanoma cell lines SK-MEL-2 and HT-144 with IC50 of 11 μM, 15 μM, 0.17 μM, 0.97 μM, 2.95 μM, 17.6 μM, 30.9 μM and 7.85 μM, respectively. [4]

細胞実験 細胞株 RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2 and HT-144 cell lines
濃度 ~100 μM
反応時間 48 hours
実験の流れ

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

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-Src(Y418) / p-FAK(Y861) p-AKT(Ser473) / AKT / PTEN / p-Src(Tyr416) VEGFR-1 / NRP-1 19383922
Immunofluorescence ATXN2L / G3BP1 E-cadherin / Vimentin 30787271
Growth inhibition assay Cell viability 28339092
In Vivo
In Vivo

A weekly i.p. injection of Oxaliplatin at 10 mg/kg to nude mice bearing hepatocellular HCCLM3 tumors significantly reduces tumor volume and apoptotic index. [6] Oxaliplatin (5mg/kg, i.v. on days 1, 5 and 9) is active on T-leukemia-lymphoma L40 AKR with T/C of 1.77. Oxaliplatin is also efficient on intracerebrally grafted L1210 leukemia, MA 16-C xenografts, B16 melanoma xenografts, Lewis lung xenografts and C26 colon carcinoma xenografts. [7] Oxaliplatin induces impairment of retrograde neuronal transport in mice. [8]

動物実験 動物モデル Human hepatocellular carcinoma xenografts HCCLM3
投与量 10 mg/kg
投与経路 A weekly i.p. injection
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

化学情報

分子量 397.29 化学式

C8H14N2O4Pt

CAS No. 61825-94-3 SDF Download Oxaliplatin SDFをダウンロードする
Smiles C1CCC(C(C1)[NH-])[NH-].C(=O)(C(=O)O)O.[Pt+2]
保管 2 years 4°C(in the dark) powder 溶液状態は不安定なので使用直前に調整してください。少量づつ分包して保管し、都度使い切る事が推奨されます。

In vitro
Batch:

Water : 2 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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よくある質問(FAQ)

質問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.

質問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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