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.
仅供研究使用。 我们不向患者出售。
化学信息
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 |
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Cas号 | 892128-60-8 |
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外观性状 | crystalline solid |
纯度 | 98% |
存储 | 3 years -20ºCpowder |
可溶性 | Soluble in DMSO |
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运输条件 | Shipped under ambient temperature as non-hazardous chemical. |
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