Home DNA Damage/DNA Repair DNA/RNA Synthesis chemical Cisplatin

연구용

Cisplatin DNA Synthesis inhibitor

제품 번호S1166

Cisplatin is an inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy.Solutions are unstable and should be fresh-prepared.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.
Cisplatin DNA/RNA Synthesis chemical Chemical Structure

화학 구조

분자량: 300.05

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품질 관리 (Quality Control)

배치: 순도: 99.84%
99.84

함께 자주 사용되는 제품 Cisplatin

Ceralasertib (AZD6738)

Explores the combined effect that potentiates the anti-tumor effects of this compound to resolve ATM-deficient non-small cell lung cancer in vivo

Berzosertib (VE-822)

Berzosertib (VX-970), when given in combination with it, enhances the efficacy of this compound in patient-derived lung tumour xenografts.

Elimusertib (BAY 1895344)

Combination treatment with BAY 1895344 and this compound achieved strong synergistic activity on the proliferation of human HT-29 colorectal cancer cells in vitro.

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
Human osteosarcoma cells (HOS, 143B, U2OS and MG‑63) Cell cycle analysis 2 μM 48 h Cisplatin treatment markedly increased the G2/M population in all cell lines. 31059083
OVC cells (A2780, TOV-112D, and cis-A2780) Cell Cytotoxicity Assay 0.5, 1, 2.5, 5, 10, 20, and 50 μM 48 h Combination of cisplatin and MEK inhibitor cobimetinib (10 nM) enhances cell death in three ovarian cancer cell lines (A2780, TOV-112D, and cis-A2780). 31057611
HCC cell lines HepG2 and Huh7 Cell viability assay 0-30 μM 48 h CD133+ HCC cells exhibit resistance to cisplatin. 31056532
Saos-2 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
OHS-50 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SK-N-MC cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 300.05 화학식

Cl2H6N2Pt

 보관 (수령일로부터) 2 years 4°C(in the dark) powder
CAS 번호 15663-27-1 SDF 다운로드 원액 보관 용액은 불안정합니다. 신선하게 준비하거나 소량의 사전 포장된 크기를 구매하십시오. 수령 즉시 재포장하십시오.
동의어 NSC 119875, Cisplatinum, cis-diamminedichloroplatinum II, CDDP, cis DDP, DDP Smiles [NH2-].[NH2-].Cl[Pt+2]Cl

용해도 (Solubility)

In vitro
배치:

DMF : 15 mg/mL

Water : Insoluble

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
One of the most widely used and most potent chemotherapeutic agents. This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).
Targets/IC50/Ki
DNA synthesis
(Tumor cells)
시험관 내(In vitro)

Cisplatin induces cytotoxic by interaction with DNA to form DNA adducts which activate several signal transduction pathways, including Erk, p53, p73, and MAPK, which culminates in the activation of apoptosis.

This compound (30 μM) treated for 6 h induces an apparent activation of Erk in HeLa cells, which is sustained over the following 14 h period. It also shows an effective antineoplastic activity by inducing tumor cells death.

It displays ability to cause renal proximal tubular cell (RPTC) apoptosis, causing cell shrinkage, a 50-fold increase in caspase 3 activity, a 4-fold increase in phosphatidylserine externalization, and 5- and 15-fold increases in chromatin condensation and DNA hypoploidy, respectively.

This chemical (800 μM) causes typical features of necrosis of RPTC after treatment for 4 hr.

생체 내(In vivo)

Cisplatin has been demonstrated to be efficient in regression tumor growth in a wide variety of animal tumors models, including head and neck cancer xenografts, cervical squamous carcinoma xenografts, testicular carcinoma xenografts, ovarian cancer xenografts, breast carcinoma xenografts, colonic carcinoma, heterotransplanted hepatoblastoma, and so on. This compound (5 mg/kg) given weekly i.v. at the day 1 and 7 induces a tumor growth inhibition (GI) of 77.5% and 85.1% of the serous xenografts Ov.Ri(C) and OVCAR-3, respectively.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/12065694/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8967349/
  • [6] https://pubmed.ncbi.nlm.nih.gov/1563830/
  • [7] https://pubmed.ncbi.nlm.nih.gov/24812268/
  • [8] https://pubmed.ncbi.nlm.nih.gov/28494534/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot ATF3 FEN1 PD-L1 / p-MEK / MEK / p-STAT3 / STAT3 LC3B-I / LC3B-II / Beclin-1 p-AMPK / AMPK / p-mTOR / mTOR
S1166-WB1
20651982
Immunofluorescence H2A.X / RPA γ-H2A.X / 53BP1 N-cadherin / E-cadherin / Vimentin LC3B
S1166-IF1
28993682
Growth inhibition assay Cell viability
S1166-viability1
26062553

임상시험 정보 (Clinical Trial Information)

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT06356155 Not yet recruiting
Urothelial Carcinoma
University of Michigan Rogel Cancer Center
 October 2024 Phase 2
NCT06393816 Not yet recruiting
Large Cell Neuroendocrine Carcinoma of the Lung
Centre Leon Berard|Groupe Français de Pneumo-Cancérologie
 May 2024 Phase 2
NCT06406465 Not yet recruiting
Carcinoma Neuroendocrine|Tumor Neuroendocrine|Tumors Neuroendocrine|Neuroendocrine; Carcinoma|Small Cell; Receptors
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 2
NCT04915183 Recruiting
Hearing Loss|Head and Neck Cancer
National Institute on Deafness and Other Communication Disorders (NIDCD)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 2

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
What is the appropriate concentration of DMF for cell culture and animal study?

답변:
It depends on the cell type. The final concentration of DMF should be better limited to less than 0.1% if possible, or below 1%. Using saline as a vehicle for it at up to 3mg/ml is recommended. It's a suspension and can be administrated via oral gavage.