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Pemetrexed disodium hemipenta hydrate
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 hemipenta hydrate图片
CAS NO:357166-30-4
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
100mg电议
500mg电议
1 g电议
5 g电议

产品名称
培美曲塞二钠水合物
LY231514 disodium hemipenta hydrate
产品介绍
Pemetrexed disodium hemipenta hydrate 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 hemipenta hydrate 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

516.41

性状

Solid

Formula

C20H24N5Na2O8.5

CAS 号

357166-30-4

中文名称

培美曲塞二钠2.5水合物

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)

溶解性数据
In Vitro: 

H2O : 100 mg/mL(193.64 mM;Need ultrasonic)

DMSO : 2 mg/mL(3.87 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9364 mL9.6822 mL19.3645 mL
5 mM0.3873 mL1.9364 mL3.8729 mL
10 mM0.1936 mL0.9682 mL1.9364 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 33.33 mg/mL (64.54 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。