Mitoxantrone

中文名稱：Mitoxantrone

目錄號：S1889 Purity: 99.14%

Mitoxantrone是一種II型拓撲異構(gòu)酶抑制劑，在HepG2和MCF-7/wt細胞中IC50分別為2.0 μM和0.42 mM。

Mitoxantrone Chemical Structure

CAS: 65271-80-9

規(guī)格	價格	庫存
100mg	658.31	現(xiàn)貨
更大包裝有超大折扣
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產(chǎn)品質(zhì)控

批次：純度： 99.14%

99.14

Mitoxantrone相關(guān)產(chǎn)品

相關(guān)靶點	Topo I Topo II Topo IV	點擊展開
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相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 DNA損傷/ DNA修復(fù)化合物庫細胞周期化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	孵育時間	活性描述
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

Mitoxantrone是一種II型拓撲異構(gòu)酶抑制劑，在HepG2和MCF-7/wt細胞中IC50分別為2.0 μM和0.42 mM。

靶點

Topo II ^[1]
(Cell-free assay)

體外研究(In Vitro)
體外研究活性	Mitoxantrone誘導DNA片段化和多聚的蛋白水解切割（ADP-核糖）聚合酶（PARP），PARP是caspases活化的標志物，證明了Mitoxantrone的的細胞毒性作用是細胞凋亡的誘導引起的。^[1] 在早幼粒細胞白血病細胞系HL60中，Mitoxantrone激活NFkappaB并刺激IkappaBalpha的降解，但在HL60/MX2細胞中沒有此作用，該細胞缺乏拓撲異構(gòu)酶II的beta同種型并表達一種截短的α亞型導致改變的亞細胞分布。^[2] Mitoxantrone以劑量依賴性方式抑制抗原呈遞細胞（APC）激活的PBMC，B淋巴細胞，或抗原特異性T細胞系（TCLs）的增殖。Mitoxantrone在低濃度誘導的外周血單個核細胞，單核細胞和樹突狀細胞凋亡，而高劑量會導致細胞裂解。^[3]

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Mitoxantrone瞬時降低HID移植瘤小鼠的增長速度，但不影響PAC120移植的小鼠。^[4] 在自發(fā)性高血壓大鼠中，Mitoxantrone導致嚴重的心肌病變，腎病和腸毒性。Mitoxantrone和鐵（III）形成牢固的2:1復(fù)合物，其中，Mitoxantrone可以充當三齒配體。^[5]

參考文獻
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/ + 展開

參考文獻

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/

+ 展開

化學信息&溶解度

分子量	444.48	分子式	C₂₂H₂₈N₄O₆
CAS號	65271-80-9	SDF	Download Mitoxantrone SDF
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 89 mg/mL ( (200.23 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 22 mg/mL ( (49.49 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑				動物體內(nèi)配方計算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	1.100mg/ml (2.47mM)	以 1 mL 工作液為例,取50μL22mg/ml的澄清DMSO儲備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請現(xiàn)配現(xiàn)用!

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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