Pemetrexed disodium hemipenta hydrate_抗叶酸和抗代谢剂_357166-30-4_Apexbio

产品名: Pemetrexed disodium hemipenta hydrate 修订日期: 6/30/2016产品说明书

化学性质

产品名:

Pemetrexed disodium hemipenta hydrate

Cas No.:

357166-30-4 分子量:

468.42 分子式:

C20H23N5NaO7+ 别名: Pemetrexed sodium hydrate

(1:2:2.5) 化学名:

tetrasodium;(2S)-2-[[4-[2-(2-amino-4-oxo-1,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]amino]pentanedioate;pentahydrate SMILES:

C1=CC(=CC=C1CCC2=CNC3=C2C(=O)N=C(N3)N)C(=O)NC(CCC(=O)O)C (=O)O.O.[Na+] 溶解性:

Soluble in Water 储存条件:

Store at -20°C 一般建议: For obtaining a higher solubility , please warm the tube at 37°C

and shake it in the ultrasonic bath for a while.Stock solution can be

stored below -20°C for several months.

运输条件:

Evaluation sample solution : ship with blue ice

All other available size: ship with RT , or blue ice upon request

生物活性

靶点 :

Apoptosis 信号通路:

Thymidylate Synthase 产品描述:

IC50 Value: 1.3nM(Ki for TS); 7.2nM(DHFR); 65nM(GARFT) Pemetrexed is approved as a first-line

treatment for advanced non-squamous non-small cell lung cancer (NSCLC) with cisplatin and as a

single agent for second-line treatment or for patients who show no disease progression after four cycles of platinum-based doublet induction chemotherapy as maintenance therapy. in vitro: The Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibition against TS, DHFR, and GARFT, respectively. In contrast, although a similar high level of inhibitory potency was observed for the parent monoglutamate against DHFR (7.0 nM), the inhibition constants (Ki) for the parent monoglutamate are significantly weaker for TS (109 nM) and GARFT(9,300 nM).The parent monoglutamate LY231514 inhibited rhTS with a Ki of 109 nM when the monoglutamated form of the substrate (6R-MTHF) (6[R]-5,l0-meth ylenetetrahydrofolate) was used. This is in good agreement with the Ki value generated earlier for rmTS (Ki= 340 nM)[1]. in vivo: pemetrexed effectively reduces kidney uptake of radiofolates not only in xenografted mice but also ina syngeneic tumor mouse model[2], Clinical trial: Phase 2 study of pemetrexed and itraconazole as second-line therapy for metastatic nonsquamous non-small-cell lung cancer is reported[3]

参考文献:

特别声明

产品仅用于研究，

不针对患者销售，望谅解。

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