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Pemetrexed.

TS、DHFR、GARFT和AICARFT抑制剂,Pemetrexed disodium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)的Ki 分别为 1.3 nM，7.2 nM 和 65 nM。

目录号: PC12529 纯度: ≥98%

CAS No. :150399-23-8

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中文名称	Pemetrexed.
中文别名	培美曲塞二钠;N-[4-[2-(2-氨基-4,7-二氢-4-氧代-1H-吡咯[2,3-d]嘧啶-5-基)乙基]苯甲酰]-L-谷氨酸二钠;Pemetrexed 抑制剂;阿伐他汀钠盐;多烯紫杉醇侧链硅化物;培美曲塞;培美曲塞二钠 Pemetrexed Disodium;培美曲塞二钠标准品;培美曲塞二钠培美酸;培美曲塞二钠盐;培美曲赛二钠;丙氨酸布立尼布;培美塞二钠;培美曲塞二纳;培美曲塞二钠二水物;培美曲塞二钠制备冻干;培美曲塞二纳制备冻干;培美曲塞二钠七水硫酸锌;培美曲塞二钠 1G;培美曲塞二钠及其杂质
英文名称	Pemetrexed
英文别名	Pemetrexed disodium;2-[4-[2-(4-Amino-2-oxo-3,5,7-triazabicyclo[4.3.0]nona-3,8,10-trien-9-yl)ethyl]benzoyl]aminopentanedioic acid disodium salt;Pemetrexed;Alimt;ALIMTA;AMN-107;LY231514 disodium;LY-231514 disodium;Nilotinib;PeMetexed DisodiuM;Pemetrexed (disodium);Pemetrexed Dinatrium;PEMETREXED SODIUM;Pemwtrexed Disodium;N-[4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid disodium salt;LY-231514;AliMta disodiuM;LY 231514 disodiuM;Rolazar;Tifolar;2PKU919BA9;Alimta (TN);Pemetrexed disodium [USAN];Pemetrexed disodium (USAN);Pemetrexed sodium hydrate;Pemetrexed disodium hydrate;disodium (2S)-2-({4-[2-(2-amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}amino)pentanedioate;Pemetrexed disodium salt;LY 231514;N-[4-[2-(2-Amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]
Cas No.	150399-23-8
分子式	C₂₀H₁₉N₅Na₂O₆
分子量	471.37
包装储存	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Pemetrexed disodium (LY231514 disodium) is an antifolate, the K_is of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

性状

Solid

IC50 & Target[1][2]

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

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.

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

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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃，, away from moisture

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

ClinicalTrial

参考文献

[1]. Shih C, et al. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23. [Information]

[2]. Anraku M, et al. Synergistic antitumor effects of regulatory T cell blockade combined with pemetrexed in murine malignantmesothelioma. J Immunol. 2010 Jul 15;185(2):956-66. [Information]

溶解度数据

体外研究:

H₂O : ≥ 100 mg/mL (212.15 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： Saline
Solubility: 100 mg/mL (212.15 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： PBS
Solubility: 50 mg/mL (106.07 mM); Clear solution; Need ultrasonic

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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