Mitoxantrone Dihydrochloride (NSC 301739)

別名: NSC-301739 2HCl, Mitozantrone 2HCl 中文名稱：米托蒽醌

目錄號：S2485 Purity: 99.86%

Mitoxantrone 2HCl是Mitoxantrone的鹽酸鹽形式。Mitoxantrone 是一種 type II topoisomerase 和 protein kinase C (PKC)的抑制劑，對于PKC的IC50值為 8.5 μM。Mitoxantrone 可抑制MCF-7/wt cells的細胞增殖，對應的IC50值為0.42 μM。Mitoxantrone 還可誘導細胞凋亡。

Mitoxantrone Dihydrochloride (NSC 301739) Chemical Structure

CAS: 70476-82-3

規(guī)格	價格	庫存
10mM (1mL in DMSO)	745.02	現(xiàn)貨
50mg	568.06	現(xiàn)貨
1g	3849.3	現(xiàn)貨
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產品質控

批次：純度： 99.86%

99.86

Mitoxantrone Dihydrochloride (NSC 301739)相關產品

相關靶點	Topo I Topo II Topo IV	點擊展開
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相關化合物庫	FDA藥物庫天然產物庫凋亡分子化合物庫 DNA損傷/ DNA修復化合物庫細胞周期化合物庫	點擊展開

細胞實驗數據示例

細胞系	實驗類型	孵育時間	活性描述
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
HL60 cells	Cytotoxicity assay	48 h	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 μM
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	Cytotoxicity 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
LoVo cells	Cytotoxicity 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 MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against human MES-SA cells after 72 hrs by MTT assay, IC50=6 nM
PC3 cancer cell	Cytotoxicity assay	144 h	Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM
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
HEK293 cells	Cytotoxicity assay	72 h	Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM
MKN45 cells	Cytotoxicity assay	144 h	Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM
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
FM3 cells	Proliferation assay	72 h	Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM
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
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	Cytotoxicity assay	48 h	Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM
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
HeLa cells	Proliferation assay	72 h	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM
NCI60 cells	Function assay	48 h	Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=47.86 nM
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
SF268 cells	Proliferation assay	48 h	Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM
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
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
SF268 cells	Cytotoxicity 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 nM
G-361 cell	Growth inhibition assay		Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM
CH1 cell	Cytotoxicity assay		Cytotoxic potency required to inhibit CH1 cell growth by 50%, IC50=2.65 nM
A549 cells	Function assay		Activity against A549 cancer cell line, IC50=3.1 nM
P388 cells	Proliferation assay		Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM
SKOV-3 cell	Cytotoxicity assay		Cytotoxic potency required to inhibit SKOV-3 cell growth 50%, IC50=5.3 nM
OVCAR-3 cell	Function assay		Antitumor activity against human ovarian OVCAR-3 cell lines, IC50=5.8 nM
MXF7 breast cell	Function assay		Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM
MCF-7 cells	Growth inhibition assay		Inhibitory activity against human tumor cell line MCF-7 breast adenocarcinoma, IC50=0.02 μM
human small-cell lung cancer	Cytotoxicity assay		Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM
UACC375 cell	Function assay		Antitumor activity against human melanoma UACC375 cell line, IC50=0.048 μM
HT1080 cell	Growth inhibition assay		Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM
HCT116 cells	Cytotoxicity assay		Cytotoxicity against human HCT116 cells by MTT assay, IC50=3.96 μM
U937 cells	Cytotoxicity assay		Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM
點擊查看更多細胞系數據

生物活性

產品描述

靶點

Topoisomerase II	PKC (Cell-free assay)
	8.5 μM

體外研究(In Vitro)
體外研究活性	Methotrexate通過主動轉運或易化擴散進入細胞和在細胞內經過多聚谷氨酸化后，會抑制二氫葉酸還原酶和二氫葉酸轉化為四氫葉酸。Methotrexate抑制嘌呤和嘧啶的從頭合成，多胺的形成以及DNA、RNA、磷脂和蛋白質的轉甲基作用。Methotrexate也會抑制胸苷酸合成酶，從而使細胞內胸苷酸不足，這可能導致抗增殖的細胞毒性作用。酶促反應被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)轉化為甲酰-AICAR，反應被AICAR甲酰基轉移酶抑制，因此導致細胞內AICAR的積累和腺苷釋放。 Methotrexate增加成纖維細胞、內皮細胞和其他細胞中腺苷的釋放。Methotrexate顯著增加腺苷的釋放，在成纖維細胞中從總嘌呤釋放(EC50, 1 nM)的4%到31%，在內皮細胞中，從24%到42%。通過暴露到受激的(fMet-Leu-Phe在0.1 μM下)中性粒細胞，Methotrexate增強的腺苷釋放，在成纖維細胞中進一步增加到總嘌呤釋放的51% (EC50, 6 nM)，在內皮細胞中增加到58%。 Methotrexate抑制免疫細胞趨藥性。Methotrexate (2.5微克/毫升)治療迅速降低多形核中性粒細胞PMNs的體外趨化反應。 Methotrexate抑制炎癥細胞因子的活性。在體外實驗中，5 nM Methotrexate抑制IL-1活性，從而抑制血管內皮細胞增殖。 Methotrexate誘導細胞凋亡。來自人類外周血液的T細胞體外活化后，Methotrexate (0.1-10 μM)會誘導其細胞凋亡。
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	p-ROS1 / ROS1 / p-STAT3 / STAT3 / p-AKT / AKT / p-ERK / ERK		30108778
	Growth inhibition assay	Cell number		24349321

體內研究(In Vivo)
體內研究活性	Methotrexate顯示出體內抗炎作用。在小鼠氣囊炎模型中，Methotrexate以劑量依賴的方式使角叉菜膠處理過的空氣袋中聚集的白血球數量減少到60% (IC50 = 0.08 毫克/千克/周)。Methotrexate (0.5 毫克/千克/周)分別增加3倍的淋巴細胞中AICAR濃度，和2倍的炎性滲出物中腺苷濃度。

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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	Recruiting	Diffuse Large B-Cell Lymphoma	CSPC ZhongQi Pharmaceutical Technology Co. Ltd.	July 10 2023	Phase 2
NCT05496894	Withdrawn	Relapsing Multiple Sclerosis	CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co. Ltd.	August 2022	Phase 2

參考文獻
[1]https://pubmed.ncbi.nlm.nih.gov/10328583/ [2]https://pubmed.ncbi.nlm.nih.gov/2476134/ [3]https://pubmed.ncbi.nlm.nih.gov/2287944/ [4]https://pubmed.ncbi.nlm.nih.gov/2476134/ [5]https://pubmed.ncbi.nlm.nih.gov/9664073/ [6]https://pubmed.ncbi.nlm.nih.gov/8254024/ [7]https://pubmed.ncbi.nlm.nih.gov/1295884/ + 展開

參考文獻

[1]https://pubmed.ncbi.nlm.nih.gov/10328583/
[2]https://pubmed.ncbi.nlm.nih.gov/2476134/
[3]https://pubmed.ncbi.nlm.nih.gov/2287944/

[4]https://pubmed.ncbi.nlm.nih.gov/2476134/
[5]https://pubmed.ncbi.nlm.nih.gov/9664073/
[6]https://pubmed.ncbi.nlm.nih.gov/8254024/
[7]https://pubmed.ncbi.nlm.nih.gov/1295884/

+ 展開

化學信息&溶解度

分子量	517.4	分子式	C₂₂H₂₉ClN₄O_6.2HCl
CAS號	70476-82-3	SDF	Download Mitoxantrone Dihydrochloride (NSC 301739) SDF
Smiles	C1=CC(=C2C(=C1NCCNCCO)C(=O)C3=C(C=CC(=C3C2=O)O)O)NCCNCCO.Cl.Cl
儲存條件(自收到貨起)	3年-20°C(避光)粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C(避光)粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (193.27 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 92 mg/mL (177.81 mM)

Ethanol : Insoluble

DMSO : 100 mg/mL ( (193.27 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 100 mg/mL (193.27 mM)

Ethanol : Insoluble

DMSO : 100 mg/mL ( (193.27 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 100 mg/mL (193.27 mM)

Ethanol : Insoluble

DMSO : 100 mg/mL ( (193.27 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 100 mg/mL (193.27 mM)

Ethanol : Insoluble

摩爾濃度計算器

體內溶解配方批次：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	Saline 該配方已經過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。	30.000mg/ml (57.98mM)	以 1 mL 工作液為例，取30mg該產品加到1ml生理鹽水（0.9% NaCL溶液）中，混合均勻使其澄清，請現(xiàn)配現(xiàn)用！

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（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 動物數量只

第二步：請輸入動物體內配方組成（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。

技術支持

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操作手冊

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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):

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Mitoxantrone Dihydrochloride (NSC 301739)

產品質控

Mitoxantrone Dihydrochloride (NSC 301739)相關產品

相關信號通路圖

細胞實驗數據示例

生物活性

化學信息&溶解度

實驗計算

技術支持