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Pentostatin_分子结构_CAS_53910-25-1)
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Pentostatin

产品号 DB00552 公司名称 DrugBank
CAS号 53910-25-1 公司网站 http://www.ualberta.ca/
分子式 C11H16N4O4 电 话 (780) 492-3111
分子量 268.26914 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 434

产品价格信息

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产品别名

标题
Pentostatin
IUPAC标准名
(8R)-3-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3H,6H,7H,8H-imidazo[4,5-d][1,3]diazepin-8-ol
IUPAC传统名
(8R)-3-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-6H,7H,8H-imidazo[4,5-d][1,3]diazepin-8-ol
商标名
Vira a Deaminase Inhibitor
Nipent
Co-V
Co-Vidarabine
Covidarabine
PD-ADI
Vidarbine
别名
2'-DCF
2'-Deoxycoformycin
2'-Dexoycoformycin
Deoxycoformycin
pentostatin

产品登记号

PubChem CID 439693
PubChem SID 46507116
CAS号 53910-25-1

产品性质

疏水性(logP) -1.1
溶解度 30 mg/mL

产品详细信息

详细说明 (English)
Item Information
Drug Groups approved; investigational
Description A potent inhibitor of adenosine deaminase. The drug is effective in the treatment of many lymphoproliferative malignancies, particularly hairy-cell leukemia. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity. [PubChem]
Indication For the treatment of hairy cell leukaemia refractory to alpha interferon.
Pharmacology Pentostatin is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic leukemia and hairy cell leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Cytotoxicity is cell cycle phase-specific (S-phase).
Toxicity LD50=128 mg/kg (mouse), side effects include lethargy, rash, fatigue, nausea and myelosuppression.
Affected Organisms
Humans and other mammals
Biotransformation Primarily hepatic, but only small amounts are metabolized.
Absorption Not absorbed orally, crosses blood brain barrier.
Half Life 5.7 hours (with a range between 2.6 and 16 hrs)
Protein Binding 4%
Elimination In man, following a single dose of 4 mg/m2 of pentostatin infused over 5 minutes, approximately 90% of the dose was excreted in the urine as unchanged pentostatin and/or metabolites as measured by adenosine deaminase inhibitory activity.
Clearance * 68 mL/min/m2
References
[Link]
External Links
Wikipedia
Drugs.com

参考文献