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Pemetrexed disodium heptahydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pemetrexed disodium heptahydrate图片
CAS NO:357166-29-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
LY231514 disodium heptahydrate
产品介绍
Pemetrexed disodium heptahydrate 是一种叶酸拮抗剂 (antifolate)。抑制胸苷酸合成酶 (TS),二氢叶酸还原酶 (DHFR) 和甘氨酰胺核苷酸甲酰转移酶 (GARFT),Ki分别为 1.3 nM,7.2 nM 和 65 nM。
生物活性

Pemetrexed disodium heptahydrate is a novelantifolate, theKivalues of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibitsthymidylate synthase(TS),dihydrofolate reductase(DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

IC50& Target

Ki: 1.3 nM (TS), 7.2 nM (DHFR), 65 nM (GARFT)[1]

体外研究
(In Vitro)

Pemetrexed (LY231514) disodium is a novel classical antifolate, the antitumor activity of which may result from simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) is one of the best substrates that is known for the enzyme FPGS (Km=1.6 μM and Vmax/Km=621). It is likely that polyglutamation and the polyglutamated metabolites of LY231514 play profound roles in determining both the selectivity and the antitumor activity of this novel agent. Whereas LY23l5l4 only moderately inhibits TS (Ki=340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (Ki=3.4 nM), making LY231514 one of the most potent folate-based TS inhibitors[1].

体内研究
(In Vivo)

The group of mice treated with PC61 plus Pemetrexed demonstrates statistically longer survival than other groups. In a survival analysis, significantly better survival is observed in the group of mice treated with PC61 plus Pemetrexed compare with those treated with PC61 alone, rat IgG plus Pemetrexed, or no treatment[2].

Clinical Trial
分子量

599.50

性状

Solid

Formula

C20H21N5O6.7H2O.2Na

CAS 号

357166-29-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)