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Mitoxantrone dihydrochloride
- английское имяMitoxantrone hydrochloride
- CAS №70476-82-3
- CBNumberCB4246424
- ФормулаC22H30Cl2N4O6
- мольный вес517.4028
- EINECS274-619-1
- номер MDLMFCD00242943
- файл Mol70476-82-3.mol
химическое свойство
Температура плавления | 203-205 C |
температура хранения | 2-8°C |
растворимость | Sparingly soluble in water, slightly soluble in methanol, practically insoluble in acetone. |
форма | Solid |
цвет | Dark Blue to Black |
Растворимость в воде | Soluble to 5 mM in water and to 75 mM in DMSO |
InChI | InChI=1S/C22H28N4O6.2ClH/c27-11-9-23-5-7-25-13-1-2-14(26-8-6-24-10-12-28)18-17(13)21(31)19-15(29)3-4-16(30)20(19)22(18)32;;/h1-4,23-30H,5-12H2;2*1H |
ИнЧИКей | ZAHQPTJLOCWVPG-UHFFFAOYSA-N |
SMILES | C1(O)=C2C(C(=O)C3=C(C2=O)C(NCCNCCO)=CC=C3NCCNCCO)=C(O)C=C1.[H]Cl.[H]Cl |
Справочник по базе данных CAS | 70476-82-3(CAS DataBase Reference) |
Словарь онкологических терминов NCI | mitoxantrone hydrochloride |
FDA UNII | U6USW86RD0 |
Словарь наркотиков NCI | mitoxantrone hydrochloride |
Предложение 65 Список | Mitoxantrone Hydrochloride |
Система регистрации веществ EPA | Mitoxantrone hydrochloride (70476-82-3) |
Коды опасности | T,T+ | |||||||||
Заявления о рисках | 46-61-26/27/28 | |||||||||
Заявления о безопасности | 53-36/37/39-45-22 | |||||||||
РИДАДР | 3249 | |||||||||
WGK Германия | 3 | |||||||||
RTECS | CB5748500 | |||||||||
Класс опасности | 6.1(b) | |||||||||
Группа упаковки | III | |||||||||
кода HS | 29146100 | |||||||||
Банк данных об опасных веществах | 70476-82-3(Hazardous Substances Data) | |||||||||
NFPA 704: |
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рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
опасность
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вредная бумага
H360:Может отрицательно повлиять на способность к деторождению или на неродившегося ребенка.
H340:Может вызывать генетические дефекты.
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оператор предупредительных мер
P201:Беречь от тепла, горячих поверхностей, искр, открытого огня и других источников воспламенения. Не курить.
P280:Использовать перчатки/ средства защиты глаз/ лица.
P308+P313:ПРИ подозрении на возможность воздействия обратиться за медицинской помощью.
Mitoxantrone dihydrochloride химические свойства, назначение, производство
Описание
Mitoxantrone hydrochloride is the first of the synthetic anthracenediones related to doxorubicin to reach the marketplace. Mitoxantrone is useful in the treatment of advanced localized and metastatic mammary carcinomas. It is reported to be less cardiotoxic than doxorubicin.Химические свойства
Dark blue, electrostatic, hygroscopic powder.Использование
analgesic, antipyreticОбщее описание
Mitoxantrone is supplied as a blue aqueous solution in 10-and 20-mg vials for IV administration in the treatment of acute lymphoid leukemia, acute myeloid leukemia, breastcancer, prostate cancer, non-Hodgkin’s lymphoma, andmultiple sclerosis. The mechanisms of resistance are thesame as those seen for the anthracyclines. The distributionhalf-life is 1.1 to 3.1 hours, and the drug has a large volumeof distribution (11 L/kg). The elimination half-life rangedfrom 23 to 215 hours, and elimination was primarily via thebile. Metabolism of the agent involves oxidation of the sidechainalcohols to give the monocarboxylic and dicarboxylicacids.Other toxicities are those seen for the anthracyclinesand include myelosuppression, nausea, vomiting, mucositis,diarrhea, and alopecia. The intense color of the parent drugand metabolites may turn the urine blue.Биологическая активность
Mitoxantrone hydrochloride (Mitoxantrone dihydrochloride) is a type II DNA topoisomerase inhibitor. Disrupts DNA synthesis and repair and induces damage by DNA cross-linking. Also inhibits PIM1 kinase (IC50 = 51 nM). Immunomodulatory, antineoplastic and chemotherapeutic agent. Also USP11 inhibitor (IC50= 3.15 μM). Induces cell death of pancreatic cancer cell lines expressing wild-type BRCA2.Клиническое использование
Mitoxantrone is used in combination with other agents during the initial treatment of acute nonlymphocytic leukemia and hormone-refractory prostate cancer. Recent studies have shown that mitoxantrone also decreases the rate of relapse and disease progression in patients with multiple sclerosis. Although too toxic for use in patients with primary progressive disease, it is available for the treatment of chronic progressive, progressive relapsing, or deteriorating relapsing-remitting multiple sclerosis.Метаболизм
Mitoxantrone excretion primarily is biliary. Both the unchanged drug and inactive metabolites resulting from N-dealkylation, deamination, and oxidation of the resultant aldehyde to the carboxylic acid are observed. Both arms of the structure can be metabolized, leading to mono- or dicarboxylic acid metabolites, which are excreted as the glucuronide conjugate. The conjugated metabolites are an intense, dark blue in color and will result in blue-green urine.Mitoxantrone dihydrochloride запасные части и сырье
Mitoxantrone dihydrochloride поставщик
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