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Oxaliplatin DNA Synthesis inhibitor

N. Cat.: S1224

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 DNA/RNA Synthesis inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 397.29

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.78%
99.78

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività PMID
Caco2 Function Assay 30/100 μM 16 h DMSO activates Nrf2 24556415
Caco2  Function Assay 3/10/30 μM 16 h DMSO increases the mRNA levels of AKR1C1, NQO1, HO-1, MRP2, andMRP3 dose-dependently 24556415
Caco2  Function Assay 30 μM 24 h DMSO induces the expression of HO-1, AKR1C, and NQO1 24556415
SW620 Growth Inhibition Assay 10-70 mg/L 24/48/72 h inhibits cell growth in both time and dose dependent manner 24646305
SW480  Growth Inhibition Assay 48 h  IC50=20.8 ug/mL 24720675
HCT116 Function Assay 2/5 µM 24/48 h suppresses survivin mRNA expression 24761411
HT-29 Growth Inhibition Assay 1 μM 0-72 h inhibits cell growth in a time dependent manner 24997451
SW480 Growth Inhibition Assay 1 μM 0-72 h inhibits cell growth in a time dependent manner 24997451
HUVEC Growth Inhibition Assay IC50=11.30 ± 1.02 μM 25307448
HEK293 Growth Inhibition Assay IC50=8.82 ± 5.59 μM 25307448
HT-29 Growth Inhibition Assay IC50>50 μM 25307448
HCT-116 Growth Inhibition Assay IC50=6.24 ± 2.97 μM 25307448
MCF-7 Growth Inhibition Assay IC50=14.24 ± 1.82 μM 25307448
HepG2 Growth Inhibition Assay IC50=14.24 ± 1.82 μM 25307448
A549 Growth Inhibition Assay IC50=51.08 ± 10.96 μM 25307448
SGC7901 Growth Inhibition Assay IC50=21.73 ± 3.08 μM 25307448
COC1 Growth Inhibition Assay IC50=46.20 ± 3.14 μM 25307448
HCT116  Growth Inhibition Assay 72 h  IC50=6.23±0.75 µg/mL 25360631
SW480 Growth Inhibition Assay 72 h  IC50=10.7±2.26 µg/mL 25360631
MIAPaCa-2 Function Assay 25 µM 24/48 h induces cleavage of PARP, caspase-9, caspase-8 and caspase-3  25444914
Panc-1 Function Assay 25 µM 24/48 h induces cleavage of PARP, caspase-9, caspase-8 and caspase-3  25444914
MIAPaCa-2 Apoptosis Assay 25 µM 24 h induces apoptosis 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
HPDE 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
MIAPaCa-2 Cell Viability Assay 25/50 μM 24/48 h inhibits proliferation of PC cells in a synergistic manner combined with WA 25444914
Panc-1 Cell Viability Assay 25/50 μM 24/48 h inhibits proliferation of PC cells in a synergistic manner combined with WA 25444914
A549/CDDP Growth Inhibition Assay IC50=18.6 ± 1.2 μM 25625243
A549 Growth Inhibition Assay IC50=5.8 ± 0.6 μM 25625243
SW480 Function Assay 10 µg/ml 24 h enhances cellular autophagic flux 25749420
SW620 Function Assay 10 µg/ml 24 h enhances cellular autophagic flux 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 increases LC3-II accumulation and decreases P62 expression 25749420
HT-29 Growth Inhibition Assay IC50=5.22 μM 25761479
SNU-175 Growth Inhibition Assay IC50=1.51 μM 25761479
COLO-320DM Growth Inhibition Assay IC50=5.38 μM 25761479
DLD-1 Growth Inhibition Assay IC50=8.65 μM 25761479
DiFi Growth Inhibition Assay IC50=10.95 μM 25761479
HCT-15 Growth Inhibition Assay IC50=8.64 μM 25761479
SCM-1 Growth Inhibition Assay IC50=17.5 μM 25789057
TMK-1 Growth Inhibition Assay IC50=22.6 μM 25789057
MKN-45 Growth Inhibition Assay IC50=14.0 μM 25789057
AGS Growth Inhibition Assay IC50=10.6 μM 25789057
S3 Growth Inhibition Assay IC50=53.5 ± 1.5 μM 25801007
SiHa Growth Inhibition Assay IC50=0.8 ± 0.1 μM 25801007
HT-29 Growth Inhibition Assay IC50=35.6 μM 26003085
DLD-1 Growth Inhibition Assay IC50=32.2 μM 26003085
HT29 Growth Inhibition Assay IC50=63 μM ± 18 26004084
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
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
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
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
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
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
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
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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 397.29 Formula

C8H14N2O4Pt

 Conservazione (Dalla data di ricezione) 2 years 4°C(in the dark) powder
N. CAS 61825-94-3 Scarica SDF Conservazione delle soluzioni stock Le soluzioni sono instabili. Preparare al momento o acquistare formati piccoli e preconfezionati. Riconfezionare al ricevimento.
Sinonimi L-OHP,NSC 266046 Smiles C1CCC(C(C1)[NH-])[NH-].C(=O)(C(=O)O)O.[Pt+2]

Solubilità (Solubility)

In vitro
Lotto:

Water : 2 mg/mL

Ethanol : Insoluble

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Caratteristiche
This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).
Targets/IC50/Ki
DNA synthesis
(RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2, HT-144 cells)
In vitro

Il principale meccanismo d'azione di Oxaliplatin è mediato dalla formazione di addotti del DNA. Questo composto induce lesioni primarie e secondarie del DNA che portano all'apoptosi cellulare. È attivo contro le linee cellulari di melanoma umano C32 e G361 con IC50 rispettivamente di 0,98 mM e 0,14 mM. Questa sostanza chimica inibisce efficacemente le linee cellulari di carcinoma della vescica RT4 e TCCSUP, la linea cellulare di carcinoma ovarico A2780, la linea cellulare di carcinoma del colon HT-29, le linee cellulari di glioblastoma U-373MG e U-87MG, e le linee cellulari di melanoma SK-MEL-2 e HT-144 con IC50 rispettivamente di 11 μM, 15 μM, 0,17 μM, 0,97 μM, 2,95 μM, 17,6 μM, 30,9 μM e 7,85 μM.

In vivo

Un'iniezione settimanale i.p. di Oxaliplatin a 10 mg/kg in topi nudi portatori di tumori epatocellulari HCCLM3 riduce significativamente il volume del tumore e l'indice apoptotico. Questo composto (5mg/kg, i.v. nei giorni 1, 5 e 9) è attivo sulla T-leucemia-linfoma L40 AKR con T/C di 1,77. È anche efficace sulla leucemia L1210 trapiantata intracerebralmente, gli xenotrapianti MA 16-C, gli xenotrapianti di melanoma B16, gli xenotrapianti polmonari di Lewis e gli xenotrapianti di carcinoma del colon C26. Questa sostanza chimica induce un'alterazione del trasporto neuronale retrogrado nei topi.

Riferimenti
  • [4] https://pubmed.ncbi.nlm.nih.gov/8261411/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15619139/
  • [6] https://pubmed.ncbi.nlm.nih.gov/19780708/
  • [7] https://pubmed.ncbi.nlm.nih.gov/2675999/
  • [8] https://pubmed.ncbi.nlm.nih.gov/23029238/
  • [9] https://pubmed.ncbi.nlm.nih.gov/24812268/

Applicazioni (Applications)

Metodi Biomarcatori Immagini PMID
Western blot VEGFR-1 / NRP-1 p-AKT(Ser473) / AKT / PTEN / p-Src(Tyr416) p-Src(Y418) / p-FAK(Y861)
S1224-WB1
18790786
Immunofluorescence E-cadherin / Vimentin ATXN2L / G3BP1
S1224-IF1
30787271
Growth inhibition assay Cell viability
S1224-viability1
28339092

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT Reclutamento Condizioni Sponsor/Collaboratori Data di inizio Fasi
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

Domande Frequenti (Frequently Asked Questions)

Domanda 1:
Is it ok to dissolve it in saline?

Risposta:
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.

Domanda 2:
Is it ok to dissolve it in DMSO?

Risposta:
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.