5-азацитидин
- английское имя5-Azacytidine
- CAS №320-67-2
- CBNumberCB4383338
- ФормулаC8H12N4O5
- мольный вес244.2
- EINECS206-280-2
- номер MDLMFCD00006539
- файл Mol320-67-2.mol
химическое свойство
| Температура плавления | 226-232 °C (dec.)(lit.) |
| альфа | 40 º (C=1, H2O 22 ºC) |
| Температура кипения | 387.12°C (rough estimate) |
| плотность | 1.4287 (rough estimate) |
| показатель преломления | 1.6590 (estimate) |
| температура хранения | -20°C |
| растворимость | Soluble in DMSO (up to 25 mg/ml), or in Water (up to 12 mg/ml). |
| пка | 13.46±0.70(Predicted) |
| форма | lyophilized powder |
| цвет | White to Off-white |
| Биологические источники | synthetic (organic) |
| Растворимость в воде | 0.5-1.0 g/100 mL at 21 ºC |
| Мерк | 14,887 |
| БРН | 620461 |
| Стабильность | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month. |
| ИнЧИКей | NMUSYJAQQFHJEW-WGDKFINWSA-N |
| LogP | -2.191 (est) |
| Справочник по базе данных CAS | 320-67-2(CAS DataBase Reference) |
| Словарь онкологических терминов NCI | azacitidine; Vidaza |
| FDA UNII | M801H13NRU |
| Словарь наркотиков NCI | azacitidine |
| Код УВД | L01BC07 |
| Предложение 65 Список | Azacitidine |
| МАИР | 2A (Vol. 50) 1990 |
| Система регистрации веществ EPA | Azacitidine (320-67-2) |
| UNSPSC Code | 41116107 |
| NACRES | NA.77 |
больше
| Коды опасности | T | |||||||||
| Заявления о рисках | 45-46-22 | |||||||||
| Заявления о безопасности | 53-22-36/37/39-45 | |||||||||
| WGK Германия | 3 | |||||||||
| RTECS | XZ3017500 | |||||||||
| F | 10-23 | |||||||||
| кода HS | 29349990 | |||||||||
| Банк данных об опасных веществах | 320-67-2(Hazardous Substances Data) | |||||||||
| Токсичность | LD50 in mice (mg/kg): 115.9 i.p.; 572.3 orally (Palm, Kensler) | |||||||||
| 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
H302：Вредно при проглатывании.
H341：Предполагается, что данное вещество вызывает генетические дефекты.
H350：Может вызывать раковые заболевания.
H372：Поражает органы в результате многократного или продолжительного воздействия.
H410：Чрезвычайно токсично для водных организмов с долгосрочными последствиями.
H360FD：Может отрицательно повлиять на способность к деторождению. Может отрицательно повлиять на неродившегося ребенка.
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оператор предупредительных мер
P202：Перед использованием ознакомиться с инструкциями по технике безопасности.
P260：Не вдыхать газ/ пары/ пыль/ аэрозоли/ дым/ туман.
P264：После работы тщательно вымыть кожу.
P273：Избегать попадания в окружающую среду.
P301+P312：ПРИ ПРОГЛАТЫВАНИИ: Обратиться за медицинской помощью при плохом самочувствии.
P308+P313：ПРИ подозрении на возможность воздействия обратиться за медицинской помощью.
5-азацитидин химические свойства, назначение, производство
Описание
5-Azacytidine is an analog of the nucleoside cytidine which can be incorporated into DNA and RNA. 5-Azacytidine acts as an epigenetic modifier by incorporating into DNA where it irreversibly binds to DNA methyltransferases, thus inhibiting their activity.Azacitidine is an antineoplastic agent launched for the treatment of myelodysplastic syndrome (MDS). MDS is a group of closely related diseases caused by abnormal blood-forming stem cells of the bone marrow. Azacitidine is indicated for the treatment of all five subtypes of MDS, which consist of refractory anemia, refractory anemia with ringed sideroblasts, refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia.
Химические свойства
White crystalline solid or powder. Soluble in dimethyl sulfoxide, slightly soluble in ethanol:water (50:50), propylene glycol, polyethylene glycol; slightly soluble in water, saturated octanol aqueous solution, 5% glucose injection, N-methyl-2-pyrrolidone, 0.9% sodium chloride injection and 5% polysorbate 80 aqueous solution; insoluble in acetone, ethanol and methyl ethyl ketone.Использование
5-Azacytidine, its incorporation into RNA alters RNA synthesis and processing, and results in inhibition of protein synthesis. It has been used as a cancer chemotherapeutic agent. It is a powerful bacteriostatic, antitumor, and mutagenic agent; it also exhibits immunosuppressive, antimitotic, radioprotective, and virostatic effects.Определение
ChEBI: A N-glycosyl-1,3,5-triazine that is 4-amino-1,3,5-triazin-2(1H)-one substituted by a beta-D-ribofuranosyl residue via a N-glycosidic linkage.Биологические функции
Azacitidine is given subcutaneously for the treatment of myelodysplastic syndrome, and serum levels generally are maximized within 30 minutes. The parent drug and its metabolites are excreted in the urine. Azacitidine is carcinogenic and teratogenic in rodents, and leukopenia, thrombocytopenia, and neutropenia are the most common reasons for drug discontinuation or dosage reduction.Общее описание
White crystalline powder.Реакции воздуха и воды
Slightly water soluble. Unstable in solution.Профиль реактивности
5-Azacytidine is sensitive to light (may discolor). 5-Azacytidine is sensitive to oxidation. 5-Azacytidine is unstable in solution. 5-Azacytidine undergoes hydrolysis in aqueous buffers. 5-Azacytidine is incompatible with strong oxidizers.Пожароопасность
Flash point data for 5-Azacytidine are not available; however, 5-Azacytidine is probably combustible.Биологическая активность
DNA methyltransferase inhibitor. Incorporates into DNA forming covalent adducts with cellular DNMT1, depleting enzyme activity. Induces demethylation and reactivation of silenced genes. Improves the efficiency of reprogramming of stem cells.Профиль безопасности
Confirmed carcinogen with experimental carcinogenic, neoplastigenic, tumorigenic data. Poison by ingestion, intravenous, and intraperitoneal routes. Human systemic effects by intravenous route: nausea, vomiting and dlarrhea, reduction in white cell count (luekopenia and agranulocytosis). An experimental teratogen. Other experimental reproductive effects. Human mutation data reported. A skin irritant. When heated to decomposition it emits toxic fumes of NOx.Канцерогенность
Azacitidine is reasonably anticipated to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in experimental animals.Перевозки
UN3249 Medicine, solid, toxic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials.Несовместимости
Azacitidine is Incompatible with oxidizers (chlorates, nitrates, peroxides, permanganates, perchlorates, chlorine, bromine, fluorine, etc.); contact may cause fires or explosions. Keep away from alkaline materials, strong bases, strong acids, oxoacids, epoxides. Contact with alkali metals, nitrides, and strong reducing agents such as hydrides may form flammable and/or toxic gases. May react with anhydrides forming acids and esters, generating noticeable heat, and also with oxoacids and carboxylic acids to form esters plus water, but the heat of reaction in the latter case typically is low. Keep away from isocyanates and epoxides; may initiate their polymerization. Azacitidine is sensitive to light and oxidation and unstable in solution. It undergoes hydrolysis in aqueous buffers.Утилизация отходов
It is inappropriate and possibly dangerous to the environment to dispose of expired or waste drugs and pharmaceuticals by flushing them down the toilet or discarding them to the trash. Household quantities of expired or waste pharmaceuticals may be mixed with wet cat litter or coffee grounds, double-bagged in plastic, discard in trash. Larger quantities shall carefully take into consideration applicable DEA, EPA, and FDA regulations. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.5-азацитидин запасные части и сырье
5-азацитидин поставщик
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