Актиномицин D химические свойства, назначение, производство
Химические свойства
Actinomycin D is a combustible, bright red crystalline solid.
Использование
Actinomycin D is the most studied member of a family of unique bicyclic depsipeptides produced by several Streptomyces species. The depsipeptides are linked by a heterocyclic benzoxazone "anchor" that gives the metabolites a highly distinctive red/orange colour. Actinomycin D exhibits potent antibiotic and antitumour activity via DNA intercalation leading to the inhibition of nucleic acid synthesis. Tumour cell death has been demonstrated to occur by apoptosis.
Показания
Dactinomycin (actinomycin D, Cosmegen) is one of a
family of chromopeptides produced by Streptomyces. It
is known to bind noncovalently to double-strand DNA
by partial intercalation, inhibiting DNA-directed RNA
synthesis. The drug is most toxic to proliferating cells,
but it is not specific for any one phase of the cell cycle.
Resistance to dactinomycin is caused by decreased ability
of tumor cells to take up and retain the drug, and it
is associated with cross-resistance to vinca alkaloids, the
anthracyclines, and certain other agents (multidrug resistance).
Общее описание
Bright red rhomboid prisms or red powder.
Реакции воздуха и воды
Water soluble.
Профиль реактивности
Actinomycin D can react with strong oxidizing agents, strong acids and strong bases.
Пожароопасность
Flash point data for Actinomycin D are not available. Actinomycin D is probably combustible.
Биологическая активность
Anti-neoplastic antibiotic. Inhibits RNA polymerase and is a potent inducer of apoptosis.
Механизм действия
Dactinomycin is cleared rapidly from plasma, does
not enter the brain, is not appreciably metabolized or
protein bound, and is gradually excreted in both bile
and urine.Virtually no drug is detected in CSF.
Клиническое использование
Dactinomycin is used in curative combined treatment
of Wilms’ tumor, Ewing’s sarcoma, rhabdomyosarcoma,
and gestational choriocarcinoma. It is active in
testicular tumors, lymphomas, melanomas, and sarcomas,
although its use in most of these malignancies has
been supplanted by other agents.
Побочные эффекты
The major side effects of dactinomycin are severe
nausea, vomiting, and myelosuppression. Mucositis, diarrhea,
alopecia, and radiation recall reactions may occur.
The drug is immunosuppressive and carcinogenic.
Возможный контакт
An antibiotic product from streptomyces, used as anticancer and veterinary drug
Перевозки
UN2811 Toxic solids, organic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials, Technical Name Required.
Методы очистки
It crystallises as bright red rhombic crystals from absolute EtOH or from MeOH/EtOH (1:3). It will also crystallise from EtOAc/cyclohexane (m 246-247o dec), CHCl3/pet ether ( m 245-246o dec), and EtOAc/MeOH/*C6H6 (m 241-243o dec). Its solubility in MeCN is 1mg/mL. [] D varies from -296o to -327o (c 0.2, MeOH). max (MeOH) 445, 240nm (log 4.43, 4.49), max (MeOH, 10N HCl, 1:1) 477nm (log 4.21) and max (MeOH, 0.1N NaOH) 458, 344, 285 (log 3.05, 4.28, 4.13). It is HIGHLY TOXIC, light sensitive and anti-neoplastic. [Bullock & Johnson, J Chem Soc 3280 1957, Beilstein 27 III/IV 9642.]
Несовместимости
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.
Актиномицин D препаратная продукция и сырье
сырьё
препарат