Mitoxantrone 2HCl
别名: NSC-301739 2HCl, Mitozantrone 2HCl 中文名称：米托蒽醌
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
产品质控
批次：
纯度：
99.86%
99.86
Mitoxantrone 2HCl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 | 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 | 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。 | ||||
|---|---|---|---|---|---|
| 靶点 |
|
| 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] |
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|---|---|---|---|---|
| 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 |
|---|---|---|---|---|---|
| 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 |
化学信息&溶解度
| 分子量 | 517.4 | 分子式 | C22H29ClN4O6.2HCl |
| 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) | |||
|
体外溶解度 |
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 (177.81 mM) Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 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
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
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。
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