Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Oxaliplatin

연구용

Oxaliplatin DNA Synthesis inhibitor

제품 번호S1224

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

화학 구조

분자량: 397.29

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품질 관리 (Quality Control)

배치: 순도: 99.78%
99.78

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 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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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 397.29 화학식

C8H14N2O4Pt

 보관 (수령일로부터) 2 years 4°C(in the dark) powder
CAS 번호 61825-94-3 SDF 다운로드 원액 보관 용액은 불안정합니다. 신선하게 준비하거나 소량의 사전 포장된 크기를 구매하십시오. 수령 즉시 재포장하십시오.
동의어 L-OHP,NSC 266046 Smiles C1CCC(C(C1)[NH-])[NH-].C(=O)(C(=O)O)O.[Pt+2]

용해도 (Solubility)

In vitro
배치:

Water : 2 mg/mL

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

특징
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)
시험관 내(In vitro)

The main mechanism of action of Oxaliplatin is mediated through the formation of DNA–adducts. This compound induces primary and secondary DNA lesions that lead to cell apoptosis. It is active against human melanoma cell lines C32 and G361 with IC50 of 0.98 mM and 0.14 mM, respectively. This chemical 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.

생체 내(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. This compound (5mg/kg, i.v. on days 1, 5 and 9) is active on T-leukemia-lymphoma L40 AKR with T/C of 1.77. It is also efficient on intracerebrally grafted L1210 leukemia, MA 16-C xenografts, B16 melanoma xenografts, Lewis lung xenografts and C26 colon carcinoma xenografts. This chemical induces impairment of retrograde neuronal transport in mice.

참조
  • [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/

적용 분야 (Applications)

방법 바이오마커 이미지 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

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
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

자주 묻는 질문 (Frequently Asked Questions)

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

답변:
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.

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

답변:
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.