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Mitoxantrone

Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.

Mitoxantrone化学構造

CAS No. 65271-80-9

サイズ 価格(税別) 在庫状況
JPY 15200 国内在庫なし(納期7~10日)

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製品安全説明書

現在のバッチを見る： S188904 DMSO] 22 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 純度： 97.45%
97.45

Mitoxantrone関連製品

シグナル伝達経路

Topoisomerase Signaling Pathways

Topoisomeraseシグナル伝達経路

Topoisomerase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
L1210 cell Cytotoxic assay 48 h Cytotoxic potency required to inhibit L1210 cell growth by 50% after cell drug contact for 48 hrs, IC50=4e-05 μM
human HL60 cells Cytotoxic assay 48 h Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 nM
A2780 cell Cytotoxic assay 96 h Cytotoxic potency required to inhibit A2780 cell growth by 50% after cell drug contact for 96 hrs, IC50=0.55 nM
HL60 human leukemia cell Cytotoxic assay 72 h Compound was tested in vitro for cytotoxicity against HL60 human leukemia cell line (72 hr exposure to compound), IC50=0.81 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 Cytotoxic assay 5 days Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=2.6 nM
MES-SA cells Proliferation assay 72 h Antiproliferative activity against MES-SA cells by MTT assay after 72 hrs, IC50=3 nM
human LoVo cancer cell Cytotoxic assay 144 h Cytotoxicity against human LoVo cancer cell line was determined after 144 hr, IC50=3.3 nM
human Daudi cells Proliferation assay 72 h Antiproliferative activity against human Daudi cells after 72 hrs by MTT assay, IC50=5 nM
human HCT116 cancer cell line Cytotoxic assay 144 h Cytotoxicity against human HCT116 cancer cell line was determined after 144 hr, 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
human PC3 cancer cell Cytotoxic assay 144 h Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM
MDR cell line K562R Cytotoxic assay 72 h Compound was tested in vitro for cytotoxicity against MDR cell line K562R (72 hr exposure to compound), IC50=7.06 nM
human Ishikawa cells Proliferation assay 72 h Antiproliferative activity against human Ishikawa cells after 72 hrs by MTT assay, IC50=0.01 μM
HEK293 cells Cytotoxic assay 72 h Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM
human MKN45 cancer cell Cytotoxic assay 144 h Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM
human LoVo cancer cell Cytotoxic assay 1 h Cytotoxicity against human LoVo cancer cell line was determined after 1 hr, IC50=0.012 μM
human FM3 cells Proliferation assay 72 h Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM
human HL60 cells Cytotoxic assay 48 h Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.016 μM
human HCT116 cells Cytotoxic 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 Cytotoxic assay 48 h Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM
CCRF-CEM cells Cytotoxic assay 48 h Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.036 μM
human HeLa cells Proliferation assay 72 h Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM
human NCI60 cells Function assay 48 h Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=0.04786 μM
human 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
human RKOp27 cells Proliferation assay 48 h Antiproliferative activity against human RKOp27 cells after 48 hrs, EC50=0.09 μM
human HeLa cells Cytotoxic assay 96 h Cytotoxicity against human HeLa cells expressing telomerase after 96 hrs by MTT assay, IC50=0.1 μM
human SKOV3 cells Proliferation assay 48 h Antiproliferative activity against human SKOV3 cells after 48 hrs, EC50=0.12 μM
human NCI-H460 cells Proliferation assay 48 h Antiproliferative activity against human NCI-H460 cells after 48 hrs, EC50=0.12 μM
SF268 cells Proliferation assay 48 h Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM
human 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
SF268 cells Cytotoxic assay 48 h Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50=0.97 μM
HepG2 cells Proliferation assay 48 h Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=11.05 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 μM
G-361 cell Cytotoxic assay Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM
CH1-cell Growth inhibition assay Concentration required to inhibit CH1-cell growth by 50%, IC50=2.65 nM
uterine sarcoma MES-SA cells Cytotoxic assay In vitro cytotoxicity against uterine sarcoma MES-SA cells, IC5=3 nM
A549 cells Function assay Tested for inhibitory activity against human tumor cell line A549 (a non small, drug resistant cell line that does not produce P-glycoprotein) of lung carcinoma using sulforhodamine B assay, IC50=3 nM
P388 cells Proliferation assay Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM
MCF-7 Growth inhibition assay In vitro inhibition of tumor cell growth in the human mammary tumor MCF-7 system, IC50=5 nM
murine L1210 sensitive cell line Function assay Anti-tumor activity against murine L1210 sensitive cell line by using MTT assay, IC50=5 nM
SKOV-3-cell Growth inhibition assay Concentration required to inhibit SKOV-3-cell growth by 50%, IC50=5.3 nM
human cell line DU145 Cytotoxic assay In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line DU145, IC50=5.6 nM
OVCAR-3 cell Function assay Inhibitory activity against OVCAR-3 cell line, IC50=5.8 nM
WiDr cell Function assay Activity against human colon carcinoma sensitive WiDr cell line, IC50=8.1 nM
MXF7 breast cell line Function assay Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM
HT-29 cell Cytotoxic assay In vitro cytotoxicity was tested against human colon adenocarcinoma HT-29 cell line, IC50=0.01 μM
CHO cell line xrs6 Cytotoxic assay Cytotoxicity against CHO cell line xrs6, IC50=0.01 μM
human HL60 cells Growth inhibition assay Growth inhibition of human HL60 cells by Almar blue assay, GI50=0.01 μM
HT-29 cells Cytotoxic assay Cytotoxicity is determined as the concentration required to inhibit the growth of human colon adenocarcinoma (HT-29) cell line, IC50=0.01 μM
SK-BR-3 cells Function assay The IC50 value was measured on human breast cancer cell line SK-BR-3, IC50=0.016 μM
human small-cell lung cancer (SCLC) Cytotoxic assay Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM
A0375 cells Function assay Inhibitory activity against human tumor cell line A0375 melanoma, IC50=0.026 μM
UA375 cells Function assay Tested for inhibitory activity against human tumor cell line UA375 of melanoma using sulforhodamine B assay, IC50=0.048 μM
HT1080 cells Function assay Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM
A549 cells Cytotoxic assay In vitro cytotoxic activity against human lung A549 cell line ( standard deviation in parenthesis), IC50=0.3 μM
MDA-MB-231 cells Proliferation assay Antiproliferative activity against human MDA-MB-231 cells, IC50=0.96 μM
MDA435/LCC6 cells Proliferation assay Antiproliferative activity against multidrug resistant MDA435/LCC6 cells by ELISA, IC50=1.442 μM
U937 cells Cytotoxic assay Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM
A549 cells Cytotoxic assay Cytotoxicity against human A549 cells by MTT assay, IC50=7.8 μM
HT-29 cell line Proliferation assay Inhibitory concentration of compound against proliferation of colon carcinoma HT-29 cell line, IC50=8 μM
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生物活性

製品説明 Mitoxantrone is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively.
Targets
Topo II [1]
(Cell-free assay)
In Vitro
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. [1] This compound 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. [2] It 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. This chemical induces apoptosis of PBMCs, monocytes and DCs at low concentrations, whereas higher doses causes cell lysis. [3]
In Vivo
In Vivo Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. [4] This compound results in the severity of the cardiac lesions and the nephropathy and the intestinal toxicity in spontaneously hypertensive rats. This chemical and iron(III) form a strong 2:1 complex, in which it may be acting as a tridentate ligand. [5]
  • https://pubmed.ncbi.nlm.nih.gov/9450803/
  • https://pubmed.ncbi.nlm.nih.gov/10940316/
  • https://pubmed.ncbi.nlm.nih.gov/16171875/
  • https://pubmed.ncbi.nlm.nih.gov/12686819/
  • https://pubmed.ncbi.nlm.nih.gov/9299365/

化学情報

分子量 444.48 化学式

C22H28N4O6
CAS No. 65271-80-9 SDF Download Mitoxantrone SDFをダウンロードする
保管

In vitro
Batch:

DMSO : 22 mg/mL ( (49.49 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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