Mitoxantrone

中文名称:Mitoxantrone

Mitoxantrone是一种II型拓扑异构酶抑制剂,在HepG2和MCF-7/wt细胞中IC50分别为2.0 μM和0.42 mM。

Mitoxantrone Chemical Structure

Mitoxantrone Chemical Structure

CAS: 65271-80-9

规格 价格 库存 购买数量
100mg 658.31 现货
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Mitoxantrone相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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 9371240
human HL60 cells Cytotoxic assay 48 h Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 nM 17962028
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 9371240
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 10479282
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 Cytotoxic 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
human LoVo cancer cell Cytotoxic 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 HCT116 cancer cell line Cytotoxic assay 144 h Cytotoxicity against human HCT116 cancer cell line was determined after 144 hr, IC50=5.8 nM 15456268
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
human PC3 cancer cell Cytotoxic assay 144 h Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM 15456268
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 10479282
human Ishikawa cells Proliferation assay 72 h Antiproliferative activity against human Ishikawa cells after 72 hrs by MTT assay, IC50=0.01 μM 25998504
HEK293 cells Cytotoxic assay 72 h Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM 24611893
human MKN45 cancer cell Cytotoxic assay 144 h Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM 15456268
human LoVo cancer cell Cytotoxic assay 1 h Cytotoxicity against human LoVo cancer cell line was determined after 1 hr, IC50=0.012 μM 15456268
human FM3 cells Proliferation assay 72 h Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM 25998504
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 22582991
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 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 Cytotoxic assay 48 h Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM 23988351
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 22582991
human HeLa cells Proliferation assay 72 h Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM 25998504
human NCI60 cells Function assay 48 h Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=0.04786 μM 18715786
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 25998504
human RKOp27 cells Proliferation assay 48 h Antiproliferative activity against human RKOp27 cells after 48 hrs, EC50=0.09 μM 23395656
human HeLa cells Cytotoxic assay 96 h Cytotoxicity against human HeLa cells expressing telomerase after 96 hrs by MTT assay, IC50=0.1 μM 18754611
human SKOV3 cells Proliferation assay 48 h Antiproliferative activity against human SKOV3 cells after 48 hrs, EC50=0.12 μM 23395656
human NCI-H460 cells Proliferation assay 48 h Antiproliferative activity against human NCI-H460 cells after 48 hrs, EC50=0.12 μM 23395656
SF268 cells Proliferation assay 48 h Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM 23395656
human 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
SF268 cells Cytotoxic 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 μM 9703471
G-361 cell Cytotoxic assay Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM 9371240
CH1-cell Growth inhibition assay Concentration required to inhibit CH1-cell growth by 50%, IC50=2.65 nM 9703471
uterine sarcoma MES-SA cells Cytotoxic assay In vitro cytotoxicity against uterine sarcoma MES-SA cells, IC5=3 nM 16169719
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 10956214
P388 cells Proliferation assay Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM 17154505
MCF-7 Growth inhibition assay In vitro inhibition of tumor cell growth in the human mammary tumor MCF-7 system, IC50=5 nM 1447730
murine L1210 sensitive cell line Function assay Anti-tumor activity against murine L1210 sensitive cell line by using MTT assay, IC50=5 nM 7699715
SKOV-3-cell Growth inhibition assay Concentration required to inhibit SKOV-3-cell growth by 50%, IC50=5.3 nM 9703471
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 10479282
OVCAR-3 cell Function assay Inhibitory activity against OVCAR-3 cell line, IC50=5.8 nM 8648600
WiDr cell Function assay Activity against human colon carcinoma sensitive WiDr cell line, IC50=8.1 nM 8960558
MXF7 breast cell line Function assay Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM 8960558
HT-29 cell Cytotoxic assay In vitro cytotoxicity was tested against human colon adenocarcinoma HT-29 cell line, IC50=0.01 μM 10411474
CHO cell line xrs6 Cytotoxic assay Cytotoxicity against CHO cell line xrs6, IC50=0.01 μM 7473578
human HL60 cells Growth inhibition assay Growth inhibition of human HL60 cells by Almar blue assay, GI50=0.01 μM 17418582
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 15456268
SK-BR-3 cells Function assay The IC50 value was measured on human breast cancer cell line SK-BR-3, IC50=0.016 μM 7699696
human small-cell lung cancer (SCLC) Cytotoxic assay Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM 8258835
A0375 cells Function assay Inhibitory activity against human tumor cell line A0375 melanoma, IC50=0.026 μM 7853345
UA375 cells Function assay Tested for inhibitory activity against human tumor cell line UA375 of melanoma using sulforhodamine B assay, IC50=0.048 μM 10956214
HT1080 cells Function assay Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM 7853345
A549 cells Cytotoxic assay In vitro cytotoxic activity against human lung A549 cell line ( standard deviation in parenthesis), IC50=0.3 μM 12036369
MDA-MB-231 cells Proliferation assay Antiproliferative activity against human MDA-MB-231 cells, IC50=0.96 μM 18296053
MDA435/LCC6 cells Proliferation assay Antiproliferative activity against multidrug resistant MDA435/LCC6 cells by ELISA, IC50=1.442 μM 17154505
U937 cells Cytotoxic assay Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM 19615900
A549 cells Cytotoxic assay Cytotoxicity against human A549 cells by MTT assay, IC50=7.8 μM 21458279
HT-29 cell line Proliferation assay Inhibitory concentration of compound against proliferation of colon carcinoma HT-29 cell line, IC50=8 μM 12031316
点击查看更多细胞系数据

生物活性

产品描述 Mitoxantrone是一种II型拓扑异构酶抑制剂,在HepG2和MCF-7/wt细胞中IC50分别为2.0 μM和0.42 mM。
靶点
Topo II [1]
(Cell-free assay)
体外研究(In Vitro)
体外研究活性 Mitoxantrone诱导DNA片段化和多聚的蛋白水解切割(ADP-核糖)聚合酶(PARP),PARP是caspases活化的标志物,证明了Mitoxantrone的的细胞毒性作用是细胞凋亡的诱导引起的。[1] 在早幼粒细胞白血病细胞系HL60中,Mitoxantrone激活NFkappaB并刺激IkappaBalpha的降解,但在HL60/MX2细胞中没有此作用,该细胞缺乏拓扑异构酶II的beta同种型并表达一种截短的α亚型导致改变的亚细胞分布。[2] Mitoxantrone以剂量依赖性方式抑制抗原呈递细胞(APC)激活的PBMC,B淋巴细胞,或抗原特异性T细胞系(TCLs)的增殖。Mitoxantrone在低浓度诱导的外周血单个核细胞,单核细胞和树突状细胞凋亡,而高剂量会导致细胞裂解。[3]
体内研究(In Vivo)
体内研究活性 Mitoxantrone瞬时降低HID移植瘤小鼠的增长速度,但不影响PAC120移植的小鼠。[4] 在自发性高血压大鼠中,Mitoxantrone导致严重的心肌病变,肾病和肠毒性。Mitoxantrone和铁(III)形成牢固的2:1复合物,其中,Mitoxantrone可以充当三齿配体。[5]

化学信息&溶解度

分子量 444.48 分子式

C22H28N4O6

CAS号 65271-80-9 SDF Download Mitoxantrone SDF
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 89 mg/mL ( (200.23 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方
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

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)

mg/kg g μL

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,: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: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: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。

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