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Pemetrexed disodium hemipenta hydrate

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Chemical Structure| 357166-30-4 同义名 : 培美曲塞二钠一水合物 ;LY-231514 Disodium Hydrate;Pemetrexed Disodium Hydrate;LY231514 disodium hemipenta hydrate
CAS号 : 357166-30-4
货号 : A708744
分子式 : C40H48N10Na4O17
纯度 : 99%
分子量 : 1032.825
MDL号 : MFCD08458870
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(1.94 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(96.82 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Pemetrexed (LY231514) disodium is a classical antifolate with novel mechanisms, exerting antitumor effects through simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) demonstrates substantial potency toward the enzyme FPGS (Km=1.6 μM and Vmax/Km=621). Polyglutamation and its metabolites likely play crucial roles in determining the selectivity and antitumor activity of Pemetrexed. While LY231514 moderately inhibits TS (Ki=340 nM, recombinant mouse), its pentaglutamate form is 100-fold more potent (Ki=3.4 nM), making Pemetrexed one of the most potent folate-based TS inhibitors [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.97mL

0.19mL

0.10mL

4.84mL

0.97mL

0.48mL

9.68mL

1.94mL

0.97mL
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.

[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.