1. Metabolic Enzyme/Protease
  2. Drug Metabolite
  3. cPrPMEDAP

cPrPMEDAP 

目录号: HY-101677
产品使用指南

cPrPMEDAP 是 GS-9219 的中间代谢产物。cPrPMEDAP 作为鸟嘌呤核苷酸类似物 PMEG 的前药发挥作用,具有抗增殖活性。cPrPMEDAP 在生理 pH 值下带负电,渗透性差。

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cPrPMEDAP Chemical Structure

cPrPMEDAP Chemical Structure

CAS No. : 182798-83-0

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生物活性

cPrPMEDAP is an intermediate metabolite of GS-9219. cpr-PMEDAP functions as a prodrug of the guanine nucleotide analog PMEG and has antiproliferative activity. cPrPMEDAP is negatively charged at physiologic pH and has poor permeability into the skin[1][2].

体外研究
(In Vitro)

cPrPMEDAP shows antiproliferative activity in SiHa cells with an EC50 of 290 nM (SiHa cells: HPV-transformed cervical carcinoma cell lines)[1].
PMEG forms an active phosphorylated metabolite, PMEG diphosphate (PMEG-DP), in cells, which inhibits the growth of various transformed cell lines due to potent inhibition of the nuclear DNA polymerases α, δ and ɛ, resulting in inhibition of DNA synthesis and/or DNA repair. In animal models, PMEG has antiproliferative effects; the utility of PMEG as an antiproliferative agent is limited by its poor cellular permeability and toxicity. cPrPMEDAP has similar antiproliferative effects in vitro and reduced toxicity in vivo but, like PMEG, is negatively charged at physiologic pH and has poor permeability into the skin[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

328.26

Formula

C11H17N6O4P

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
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  • 稀释计算器

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产品名称:
cPrPMEDAP
目录号:
HY-101677
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