Mitoxantrone 2HCl

Mitoxantrone 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.

CAS No. 70476-82-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
100mg	JPY 37000	国内在庫あり
1g	JPY 100500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（49）

製品安全説明書

現在のバッチを見る：純度： 99.94%

99.94

Mitoxantrone 2HCl関連製品

関連ターゲット	Topo I Topo II Topo IV	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

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	Incubation Time	活性情報	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	9371240
HL60 cells	Cytotoxicity assay	48 h	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 μM	17962028
human HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay, IC50=2.5 nM	22944121
human K562 cells	Cytotoxicity assay	5 days	Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=2.6 nM	18076140
MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against MES-SA cells by MTT assay after 72 hrs, IC50=3 nM	16824751
LoVo cells	Cytotoxicity assay	144 h	Cytotoxicity against human LoVo cancer cell line was determined after 144 hr, IC50=3.3 nM	15456268
human Daudi cells	Proliferation assay	72 h	Antiproliferative activity against human Daudi cells after 72 hrs by MTT assay, IC50=5 nM	25998504
human MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against human MES-SA cells after 72 hrs by MTT assay, IC50=6 nM	25998504
PC3 cancer cell	Cytotoxicity assay	144 h	Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM	15456268
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	9371240
HEK293 cells	Cytotoxicity assay	72 h	Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM	24611893
MKN45 cells	Cytotoxicity assay	144 h	Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM	15456268
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	21444205
FM3 cells	Proliferation assay	72 h	Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM	25998504
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	21444205
human HCT116 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.025 μM	25998504
NCI-H460 cells	Cytotoxicity assay	48 h	Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM	23988351
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	22582991
HeLa cells	Proliferation assay	72 h	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM	25998504
NCI60 cells	Function assay	48 h	Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=47.86 nM	18715786
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	25998504
SF268 cells	Proliferation assay	48 h	Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM	23395656
KB/HeLa cells	Proliferation assay	48 h	Antiproliferative activity against human KB/HeLa cells after 48 hrs, EC50=0.36 μM	23395656
K562 cells	Growth inhibition assay	72 h	Growth inhibition of human K562 cells after 72 hrs by MTS method, IC50=0.42 μM	18258442
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	17335189
SF268 cells	Cytotoxicity assay	48 h	Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50=0.97 μM	17962028
HepG2 cells	Proliferation assay	48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=11.05 μM	24794747
MDA435/LCC6 cells	Proliferation assay		Antiproliferative activity against MDA435/LCC6 cells by ELISA, IC50=0.35 nM	17154505
A2780-cell	Growth inhibition assay		Concentration required to inhibit A2780-cell growth by 50%, IC50=0.55 nM	9703471
G-361 cell	Growth inhibition assay		Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM	9371240
CH1 cell	Cytotoxicity assay		Cytotoxic potency required to inhibit CH1 cell growth by 50%, IC50=2.65 nM	9371240
A549 cells	Function assay		Activity against A549 cancer cell line, IC50=3.1 nM	8960558
P388 cells	Proliferation assay		Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM	17154505
SKOV-3 cell	Cytotoxicity assay		Cytotoxic potency required to inhibit SKOV-3 cell growth 50%, IC50=5.3 nM	9371240
OVCAR-3 cell	Function assay		Antitumor activity against human ovarian OVCAR-3 cell lines, IC50=5.8 nM	8960558
MXF7 breast cell	Function assay		Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM	8960558
MCF-7 cells	Growth inhibition assay		Inhibitory activity against human tumor cell line MCF-7 breast adenocarcinoma, IC50=0.02 μM	7853345
human small-cell lung cancer	Cytotoxicity assay		Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM	8258835
UACC375 cell	Function assay		Antitumor activity against human melanoma UACC375 cell line, IC50=0.048 μM	8960558
HT1080 cell	Growth inhibition assay		Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM	7853345
HCT116 cells	Cytotoxicity assay		Cytotoxicity against human HCT116 cells by MTT assay, IC50=3.96 μM	20951582
U937 cells	Cytotoxicity assay		Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM	19615900
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Mitoxantrone 2HCl is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.

Targets

Topoisomerase II ^[1]	PKC ^[7] (Cell-free assay)
	8.5 μM

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] 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. ^[2] 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. ^[3]
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK		30108778
	Growth inhibition assay	Cell number		24349321

In Vivo
In Vivo	Mitoxantrone transiently decreases the growth rate of HID xenografts in mice but does not affect that of PAC120 xenografts. ^[4] 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. ^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06156761	Not yet recruiting	Breast Cancer	Cancer Institute and Hospital Chinese Academy of Medical Sciences\|CSPC Ouyi Pharmaceutical Co. Ltd.	November 28 2023	Not Applicable
NCT05875428	Not yet recruiting	Diffuse Large B-Cell Lymphoma	CSPC ZhongQi Pharmaceutical Technology Co. Ltd.	June 1 2023	Phase 2
NCT05496894	Withdrawn	Relapsing Multiple Sclerosis	CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co. Ltd.	August 2022	Phase 2

参考
[1] Seitz M. Curr Opin Rheumatol, 1999, 11(3), 226-232. [2] Hirata S, et al. Arthritis Rheum, 1989 , 32(9), 1065-1073. [3] Segal R, et al. Semin Arthritis Rheum, 1990, 20(3), 190-200. [4] Hirata S, et al. Arthritis Rheum, 1989, 32(9), 1065-1073. [5] Genestier L, et al. J Clin Invest, 1998, 102(2), 322-328. [6] Cronstein BN, et al. J Clin Invest, 1993, 92(6):2675-2682. [7] N Takeuchi, et al. J Biochem. 1992 Dec;112(6):762-7. + 展開

参考

+ 展開

化学情報

分子量	517.4	化学式	C₂₂H₂₉ClN₄O_6.2HCl
CAS No.	70476-82-3	SDF	Download Mitoxantrone 2HCl SDFをダウンロードする
Smiles	C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 104 mg/mL ( (201.0 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 : 104 mg/mL

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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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。

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):