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Oxaliplatin DNA 합성 억제제

Name: Oxaliplatin
Brand: Selleck Chemicals
SKU: S1224
Rating: 5 (277 reviews)

제품 번호S1224

Oxaliplatin은 autophagy를 활성화하는 DNA 알킬화제입니다. Oxaliplatin은 RT4, TCCSUP, A2780, HT-29, U-373MG, U-87MG, SK-MEL-2 및 HT-144 세포에서 DNA 부가물을 형성하여 DNA 합성을 억제합니다.용액은 불안정하므로 신선하게 준비해야 합니다. DMSO는 백금 기반 약물을 용해하는 데 권장되지 않으며, 이는 약물 비활성화를 쉽게 초래할 수 있습니다.

Oxaliplatin DNA/RNA Synthesis 억제제 Chemical Structure

화학 구조

분자량: 397.29

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품질 관리

배치: 순도: 99.78%

99.78

관련 타겟	HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF
기타 DNA/RNA Synthesis 억제제	CX-5461 (Pidnarulex) B02 SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279

세포 배양, 처리 및 작업 농도

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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

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

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)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

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

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)	Oxaliplatin의 주요 작용 메커니즘은 DNA-부가물 형성을 통해 매개됩니다. 이 화합물은 세포 사멸로 이어지는 1차 및 2차 DNA 손상을 유도합니다. 이는 인간 흑색종 세포주 C32 및 G361에 대해 각각 0.98 mM 및 0.14 mM의 IC50을 가지며 활성을 나타냅니다. 이 화학물질은 방광암 세포주 RT4 및 TCCSUP, 난소암 세포주 A2780, 결장암 세포주 HT-29, 교모세포종 세포주 U-373MG 및 U-87MG, 흑색종 세포주 SK-MEL-2 및 HT-144를 각각 11 μM, 15 μM, 0.17 μM, 0.97 μM, 2.95 μM, 17.6 μM, 30.9 μM 및 7.85 μM의 IC50으로 효과적으로 억제합니다.
생체 내(In vivo)	HCCLM3 간세포암종 종양을 이식한 누드 마우스에 Oxaliplatin을 10 mg/kg 주 1회 복강내 주사하면 종양 부피와 세포 사멸 지수가 유의하게 감소합니다. 이 화합물(5mg/kg, 1, 5, 9일차에 정맥 주사)은 L40 AKR T-백혈병-림프종에 대해 T/C 1.77로 활성을 나타냅니다. 또한 뇌내 이식된 L1210 백혈병, MA 16-C 이종이식편, B16 흑색종 이종이식편, 루이스 폐암 이종이식편 및 C₂₆ 결장암 이종이식편에도 효과적입니다. 이 화학물질은 마우스에서 역행성 신경 수송 장애를 유도합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/9834817/ [2] https://pubmed.ncbi.nlm.nih.gov/11142694/ [3] https://pubmed.ncbi.nlm.nih.gov/18043128/ [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

방법	바이오마커	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

임상시험 정보

(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

기술 지원

취급 설명서

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자주 묻는 질문

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.

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):