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LY2334737 编号 : 16123040

化学信息

产品英文名称LY2334737
Iupac 化学名称LY2334737 
同义词LY 2334737; LY-2334737; gemcitabine prodrug 
英文同义词LY 2334737; LY-2334737; gemcitabine prodrug 
分子式C17H25F2N3O5 
分子量389.39 
InChiKey
InChi
Cas892128-60-8

技术数据

外观crystalline solid 
纯度98% 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature as non-hazardous chemical. 
质量控制

产品详情

LY2334737 is an orally available valproic acid ester of gemcitabine, a broad-spectrum antimetabolite with antineoplastic activity. LY2334737 is hydrolyzed by carboxylesterase 2 (CES2) and releases gemcitabine systemically over a period of time consistent with formation rate-limited kinetics. In turn, gemcitabine is converted into the active metabolites difluorodeoxycytidine diphosphate and triphosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA replication; dFdCTP is incorporated into DNA, resulting in premature termination of DNA replication and eventually the induction of apoptosis. Compared to gemcitabine, this prodrug is able to avoid hydrolysis in enterocytes and the portal circulation thus avoiding first pass metabolism and increasing systemic gemcitabine availability. 

结构

16123040 - LY2334737 | CAS 892128-60-8

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