Mitoxantrone 2HCl

别名: NSC-301739 2HCl, Mitozantrone 2HCl 中文名称：米托蒽醌

目录号：S2485 Purity: 99.86%

Mitoxantrone 2HCl是Mitoxantrone的盐酸盐形式。Mitoxantrone 是一种 type II topoisomerase 和 protein kinase C (PKC)的抑制剂，对于PKC的IC50值为 8.5 μM。Mitoxantrone 可抑制MCF-7/wt cells的细胞增殖，对应的IC50值为0.42 μM。Mitoxantrone 还可诱导细胞凋亡。

Mitoxantrone 2HCl Chemical Structure

CAS: 70476-82-3

规格	价格	库存
10mM (1mL in DMSO)	RMB 745.02	现货
50mg	RMB 568.06	现货
1g	RMB 3849.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

客户使用Selleck的Mitoxantrone 2HCl发表文献49篇

产品质控

批次：纯度： 99.86%

99.86

Mitoxantrone 2HCl相关产品

相关靶点	Topo I Topo II Topo IV	点击展开
相关产品	Betulinic acid (S)-10-Hydroxycamptothecin Beta-Lapachone Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Pixantrone Maleate Genz-644282 Hydroxy Camptothecine Rubitecan	点击展开
相关化合物库	FDA药物库天然产物库凋亡分子化合物库 DNA损伤/ DNA修复化合物库细胞周期化合物库	点击展开

Topoisomerase抑制剂选择性比较

细胞实验数据示例

细胞系	实验类型	孵育时间	活性描述	文献信息
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
点击查看更多细胞系数据

生物活性

产品描述

靶点

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

体外研究(In Vitro)
体外研究活性	Methotrexate通过主动转运或易化扩散进入细胞和在细胞内经过多聚谷氨酸化后，会抑制二氢叶酸还原酶和二氢叶酸转化为四氢叶酸。Methotrexate抑制嘌呤和嘧啶的从头合成，多胺的形成以及DNA、RNA、磷脂和蛋白质的转甲基作用。Methotrexate也会抑制胸苷酸合成酶，从而使细胞内胸苷酸不足，这可能导致抗增殖的细胞毒性作用。酶促反应被Methotrexate的多聚谷氨酸化最有效抑制的是5-氨基-4-甲酰胺咪唑核糖核苷酸(AICAR)转化为甲酰-AICAR，反应被AICAR甲酰基转移酶抑制，因此导致细胞内AICAR的积累和腺苷释放。^[1] Methotrexate增加成纤维细胞、内皮细胞和其他细胞中腺苷的释放。Methotrexate显著增加腺苷的释放，在成纤维细胞中从总嘌呤释放(EC50, 1 nM)的4%到31%，在内皮细胞中，从24%到42%。通过暴露到受激的(fMet-Leu-Phe在0.1 μM下)中性粒细胞，Methotrexate增强的腺苷释放，在成纤维细胞中进一步增加到总嘌呤释放的51% (EC50, 6 nM)，在内皮细胞中增加到58%。^[2] Methotrexate抑制免疫细胞趋药性。Methotrexate (2.5微克/毫升)治疗迅速降低多形核中性粒细胞PMNs的体外趋化反应。^[3] Methotrexate抑制炎症细胞因子的活性。在体外实验中，5 nM Methotrexate抑制IL-1活性，从而抑制血管内皮细胞增殖。^[4] Methotrexate诱导细胞凋亡。来自人类外周血液的T细胞体外活化后，Methotrexate (0.1-10 μM)会诱导其细胞凋亡。^[5]
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK		30108778
	Growth inhibition assay	Cell number		24349321

体内研究(In Vivo)
体内研究活性	Methotrexate显示出体内抗炎作用。在小鼠气囊炎模型中，Methotrexate以剂量依赖的方式使角叉菜胶处理过的空气袋中聚集的白血球数量减少到60% (IC50 = 0.08 毫克/千克/周)。Methotrexate (0.5 毫克/千克/周)分别增加3倍的淋巴细胞中AICAR浓度，和2倍的炎性渗出物中腺苷浓度。^[6]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (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

参考文献
[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. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	517.4	分子式	C₂₂H₂₉ClN₄O_6.2HCl
CAS号	70476-82-3	SDF	Download Mitoxantrone 2HCl SDF
Smiles	C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (193.27 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : 92 mg/mL

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

* 姓名 请输入您的姓名

* 邮箱 请输入您的邮箱地址 请输入一个有效的邮箱地址

电话

* 留言内容 请写点东西给我们

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):