Mitoxantrone 2HCl

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(yīng)的IC50值為0.42 μM。Mitoxantrone 還可誘導(dǎo)細胞凋亡。

Mitoxantrone 2HCl 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(chǎn)品質(zhì)控

批次：純度： 99.86%

99.86

Mitoxantrone 2HCl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	FDA藥物庫天然產(chǎn)物庫凋亡分子化合物庫 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	文獻信息
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
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生物活性

產(chǎn)品描述

靶點

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

體外研究(In Vitro)
體外研究活性	Methotrexate通過主動轉(zhuǎn)運或易化擴散進入細胞和在細胞內(nèi)經(jīng)過多聚谷氨酸化后，會抑制二氫葉酸還原酶和二氫葉酸轉(zhuǎn)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(zhì)的轉(zhuǎn)甲基作用。Methotrexate也會抑制胸苷酸合成酶，從而使細胞內(nèi)胸苷酸不足，這可能導(dǎo)致抗增殖的細胞毒性作用。酶促反應(yīng)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(zhuǎn)化為甲酰-AICAR，反應(yīng)被AICAR甲?；D(zhuǎn)移酶抑制，因此導(dǎo)致細胞內(nèi)AICAR的積累和腺苷釋放。^[1] Methotrexate增加成纖維細胞、內(nèi)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(nèi)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(nèi)皮細胞中增加到58%。^[2] 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(yīng)。^[3] 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(nèi)皮細胞增殖。^[4] Methotrexate誘導(dǎo)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(dǎo)其細胞凋亡。^[5]
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(nèi)研究(In Vivo)
體內(nèi)研究活性	Methotrexate顯示出體內(nèi)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(shù)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。^[6]

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] 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

參考文獻

[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

化學(xué)信息&溶解度

分子量	517.4	分子式	C₂₂H₂₉ClN₄O_6.2HCl
CAS號	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
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 : 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(nèi)溶解度
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

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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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 2HCl

產(chǎn)品質(zhì)控

Mitoxantrone 2HCl相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實驗計算

技術(shù)支持