연구용

Mitoxantrone Dihydrochloride (NSC 301739) PKC/Topoisomerase II 억제제

제품 번호: S2485

Mitoxantrone 2HCl은 Mitoxantrone의 염산염입니다. Mitoxantrone은 type II topoisomerase 및 protein kinase C (PKC) 억제제로, PKC에 대한 IC50은 8.5 μM입니다. Mitoxantrone은 MCF-7/wt 세포의 증식 성장을 0.42 μM의 IC50으로 억제합니다. Mitoxantrone은 또한 apoptosis를 유도합니다.
Mitoxantrone Dihydrochloride (NSC 301739) Topoisomerase 억제제 Chemical Structure

화학 구조

분자량: 517.4

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품질 관리 (Quality Control)

배치: 순도: 99.94%
99.94

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
L1210 cell Cytotoxicity assay 48 h Cytotoxic potency required to inhibit L1210 cell growth by 50% after cell drug contact for 48 hrs, IC50=4e-05 μM
HL60 cells Cytotoxicity assay 48 h Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 μM
MDA435/LCC6 cells Proliferation assay Antiproliferative activity against MDA435/LCC6 cells by ELISA, IC50=0.35 nM
A2780-cell Growth inhibition assay Concentration required to inhibit A2780-cell growth by 50%, IC50=0.55 nM
G-361 cell Growth inhibition assay Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM
human HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay, IC50=2.5 nM
human K562 cells Cytotoxicity assay 5 days Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=2.6 nM
CH1 cell Cytotoxicity assay Cytotoxic potency required to inhibit CH1 cell growth by 50%, IC50=2.65 nM
MES-SA cells Proliferation assay 72 h Antiproliferative activity against MES-SA cells by MTT assay after 72 hrs, IC50=3 nM
A549 cells Function assay Activity against A549 cancer cell line, IC50=3.1 nM
LoVo cells Cytotoxicity assay 144 h Cytotoxicity against human LoVo cancer cell line was determined after 144 hr, IC50=3.3 nM
P388 cells Proliferation assay Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM
human Daudi cells Proliferation assay 72 h Antiproliferative activity against human Daudi cells after 72 hrs by MTT assay, IC50=5 nM
SKOV-3 cell Cytotoxicity assay Cytotoxic potency required to inhibit SKOV-3 cell growth 50%, IC50=5.3 nM
OVCAR-3 cell Function assay Antitumor activity against human ovarian OVCAR-3 cell lines, IC50=5.8 nM
human MES-SA cells Proliferation assay 72 h Antiproliferative activity against human MES-SA cells after 72 hrs by MTT assay, IC50=6 nM
PC3 cancer cell Cytotoxicity assay 144 h Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM
MXF7 breast cell Function assay Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM
HT-29 cell Cytotoxicity assay 144 h Cytotoxic potency required to inhibit HT-29 cell growth by 50% after cell drug contact for 144 hrs, IC5=0.01 μM
HEK293 cells Cytotoxicity assay 72 h Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM
MKN45 cells Cytotoxicity assay 144 h Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM
MES-SA cells Cytotoxicity assay 72 h Cytotoxicity against human MES-SA cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.012 μM
FM3 cells Proliferation assay 72 h Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM
MCF-7 cells Growth inhibition assay Inhibitory activity against human tumor cell line MCF-7 breast adenocarcinoma, IC50=0.02 μM
human small-cell lung cancer Cytotoxicity assay Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM
human HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.022 μM
human HCT116 cells Proliferation assay 72 h Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.025 μM
NCI-H460 cells Cytotoxicity assay 48 h Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM
CCRF-CEM cells Cytotoxicity assay 48 h Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.036 μM
HeLa cells Proliferation assay 72 h Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM
NCI60 cells Function assay 48 h Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=47.86 nM
UACC375 cell Function assay Antitumor activity against human melanoma UACC375 cell line, IC50=0.048 μM
HT1080 cell Growth inhibition assay Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM
MES-SA/Dx5 cells Proliferation assay 72 h Antiproliferative activity against human MES-SA/Dx5 cells after 72 hrs by MTT assay, IC50=0.073 μM
SF268 cells Proliferation assay 48 h Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM
KB/HeLa cells Proliferation assay 48 h Antiproliferative activity against human KB/HeLa cells after 48 hrs, EC50=0.36 μM
K562 cells Growth inhibition assay 72 h Growth inhibition of human K562 cells after 72 hrs by MTS method, IC50=0.42 μM
MDA-MB-231 cells Proliferation assay 72 h Antiproliferative activity against human MDA-MB-231 cells by WST-1 method after 72 hrs, IC50=0.96 μM
SF268 cells Cytotoxicity assay 48 h Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50=0.97 μM
HCT116 cells Cytotoxicity assay Cytotoxicity against human HCT116 cells by MTT assay, IC50=3.96 μM
U937 cells Cytotoxicity assay Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM
HepG2 cells Proliferation assay 48 h Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=11.05 μM
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 517.4 화학식

C22H29ClN4O6.2HCl

보관 (수령일로부터) 3 years-20°C(in the dark) powder
CAS 번호 70476-82-3 SDF 다운로드 원액 보관 용액은 불안정합니다. 신선하게 준비하거나 소량의 사전 포장된 크기를 구매하십시오. 수령 즉시 재포장하십시오.
동의어 NSC-301739 2HCl, Mitozantrone 2HCl Smiles C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl

용해도 (Solubility)

In vitro
배치:

DMSO : 104 mg/mL (201.0 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 104 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)

Targets/IC50/Ki
Topoisomerase II
PKC
(Cell-free assay)
8.5 μM
시험관 내(In vitro)

Mitoxantrone induces DNA fragmentation and the proteolytic cleavage of poly(ADP-ribose) polymerase (PARP), a marker of the activation of caspases, in all the patients studied, demonstrating that the cytotoxic effect of mitoxantrone is due to induction of apoptosis. Mitoxantrone activates NFkappaB and stimulates IkappaBalpha degradation in the promyelocytic leukemia cell line HL60 but not in the variant cells, HL60/MX2 cells, which lack the beta isoform of topoisomerase II and express a truncated alpha isoform that results in an altered subcellular distribution. Mitoxantrone inhibits proliferation of activated PBMCs, B lymphocytes, or antigen-specific T-cell lines (TCLs) stimulated on antigen-presenting cells (APCs) in a dose-dependent manner. Mitoxantrone induces apoptosis of PBMCs, monocytes and DCs at low concentrations, whereas higher doses causes cell lysis.

생체 내(In vivo)

Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. Mitoxantrone results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. Mitoxantrone and iron(III) form a strong 2:1 complex, in which mitoxantrone may be acting as a tridentate ligand.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/2476134/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9664073/
  • [6] https://pubmed.ncbi.nlm.nih.gov/8254024/
  • [7] https://pubmed.ncbi.nlm.nih.gov/1295884/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK
S2485-WB1
30108778
Growth inhibition assay Cell number
S2485-viability1
24349321

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2026-06-29)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT02724163 ACTIVE_NOT_RECRUITING
Acute Myeloid Leukaemia
University of Birmingham
2016-04 PHASE3
NCT07754799 NOT_YET_RECRUITING
Acute Myeloid Leukemia (AML)
Institute of Hematology & Blood Diseases Hospital, China
2026-09-30 PHASE2
NCT04293562 RECRUITING
Acute Myeloid Leukemia
Children's Oncology Group
2020-07-21 PHASE3
NCT03591510 ACTIVE_NOT_RECRUITING
FLT3-mutated Acute Myeloid Leukemia
Novartis Pharmaceuticals
2019-03-13 PHASE2
NCT05848687 RECRUITING
Lymphoblastic Leukemia
Tanja Andrea Gruber
2023-11-03 PHASE1; PHASE2
NCT06221683 RECRUITING
AML, Childhood; Acute Myeloid Leukemia
Children's Hospital of Soochow University
2024-01-01 PHASE2