Pemetrexed disodium

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Pemetrexed disodium

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。

CAS NO:

150399-23-8

包装与价格：

包装	价格(元)
10 mM * 1 mL in Water	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议
1 g	电议

产品名称

培美曲塞二钠盐
LY231514 disodium

产品介绍

Pemetrexed disodium (LY231514 disodium) 是一种叶酸拮抗剂 (antifolate)。Pemetrexed disodium 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) 的K_i分别为 1.3 nM，7.2 nM 和 65 nM。

生物活性

Pemetrexed disodium (LY231514 disodium) is anantifolate, theK_is of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibitsthymidylate synthase(TS),dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively^[1].

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 (K_m=1.6 μM and V_max/K_m=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 (K_i=340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (K_i=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

471.37

性状

Solid

Formula

C₂₀H₁₉N₅Na₂O₆

CAS 号

150399-23-8

中文名称

培美曲塞二钠盐

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(212.15 mM)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.1215 mL	10.6074 mL	21.2148 mL
5 mM	0.4243 mL	2.1215 mL	4.2430 mL
10 mM	0.2121 mL	1.0607 mL	2.1215 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： Saline
Solubility: 100 mg/mL (212.15 mM); Clear solution; Need ultrasonic
2.
请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (106.07 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。