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药品详细

Plicamycin(普卡霉素)

化学结构式图
中文名
普卡霉素
英文名
Plicamycin
分子式
C52H76O24
化学名
(2S,3S)-3-[(1S,3S,4R)-3,4-dihydroxy-1-methoxy-2-oxopentyl]-2-{[(2S,4R,5R,6R)-4-{[(2S,4R,5S,6R)-4-{[(2S,4S,5R,6R)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy}-5-hydroxy-6-methyloxan-2-yl]oxy}-5-hydroxy-6-methyloxan-2-yl]oxy}-6-{[(2S,4R,5R,6R)-4-{[(2S,4R,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy}-5-hydroxy-6-methyloxan-2-yl]oxy}-8,9-dihydroxy-7-methyl-1,2,3,4-tetrahydroanthracen-1-one
分子量
Average: 1085.1454
Monoisotopic: 1084.47265336
CAS号
18378-89-7
ATC分类
L01D 细胞毒素抗生素及相关物质
药物类型
small molecule
阶段
approved, withdrawn
商品名
同义名
基本介绍

Plicamycin is an antineoplastic antibiotic produced by Streptomyces plicatus. It has been used in the treatment of testicular cancer, Paget’s disease of bone, and, rarely, the management of hypercalcemia. The manufacturer discontinued plicamycin in 2000.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Wohlert SE, Kunzel E, Machinek R, Mendez C, Salas JA, Rohr J: The structure of mithramycin reinvestigated. J Nat Prod. 1999 Jan;62(1):119-21. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication For the treatment of testicular cancer, as well as hypercalcemia and hypercalciuria associated with a variety of advanced forms of cancer.
    Pharmacodynamics Plicamycin is lethal to Hela cells in 48 hours at concentrations as low as 0.5 micrograms per milliliter of tissue culture medium. Plicamycin has shown significant anti-tumor activity against experimental leukemia in mice when administered intraperitoneally.
    Mechanism of action Plicamycin is presumed to inhibit cellular and enzymic RNA synthesis by forming a complex with DNA. Plicamycin may also lower calcium serum levels by inhibiting the effect of parathyroid hormone upon osteoclasts or by blocking the hypercalcemic action of pharmacologic doses of vitamin D.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding There is no evidence of protein binding, nor is there any evidence of metabolism of the carbohydrate moiety of the drug to carbon dioxide and water with loss through respiration.
    Metabolism
    Not Available
    Route of elimination Radioautography studies with 3H-labeled plicamycin in mice show that the greatest concentrations of the isotope are in the Kupffer cells of the liver and cells of the renal tubules. Plicamycin is rapidly cleared from the blood within the first 2 hours and excretion is also rapid. 67% percent of measured excretion occurs within 4 hours, 75% within 8 hours, and 90% is recovered in the first 24 hours after injection.
    Half life Not Available
    Clearance Not Available
    Toxicity The most important form of toxicity associated with the use of plicamycin consists of a dose-related bleeding syndrome which usually begins with an episode of epistaxis. Plicamycin crosses the blood-brain barrier; the concentration found in brain tissue is low but it persists longer than in other tissues.
    Affected organisms Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 181.5 °C PhysProp
    Predicted Properties
    Property Value Source
    water solubility 1.30e+00 g/l ALOGPS
    logP -0.23 ALOGPS
    logP 2.07 ChemAxon
    logS -2.9 ALOGPS
    pKa (strongest acidic) 8.49 ChemAxon
    pKa (strongest basic) -3.6 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 24 ChemAxon
    hydrogen donor count 11 ChemAxon
    polar surface area 358.2 ChemAxon
    rotatable bond count 15 ChemAxon
    refractivity 257.01 ChemAxon
    polarizability 114.41 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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