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Pemetrexed disodium

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Chemical Structure| 150399-23-8 同义名 : 培美曲塞二钠 ;LY231514 disodium
CAS号 : 150399-23-8
货号 : A206176
分子式 : C20H19N5Na2O6
纯度 : 99.9%
分子量 : 471.374
MDL号 : -
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 :

H2O: 100 mg/mL(212.15 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • DHFR

    DHFR, Ki:7.2 nM
描述 Pemetrexed disodium is a potent new antifolate which inhibits many folate-dependent reactions that are essential for cell proliferation. Its primary target is thymidylate synthase but it also inhibits folate-dependent enzymes involved in purine synthesis. In the majority of clinical trials of pemetrexed, the dose-limiting toxic effect is neutropenia; other side-effects are mostly gastrointestinal. As a single agent pemetrexed has shown good activity against non-small-cell lung cancer, squamous-cell carcinoma of head and neck, colon cancer, and breast cancer, and it appears to be particularly active in combination with cisplatin against non-small-cell lung cancer and mesothelioma[3]. Pemetrexed disodium is an antifolate, the Kis 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[4]. As a single agent, pemetrexed exhibits a moderate toxicity profile at a dose of 500 mg/m(2) by 10-minute infusion once every 21 days with myelosuppression being the dose-limiting toxicity[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
211H Growth Inhibition Assay IC50=0.07±0.01 μM 24714722
A459 1/2/4 μM Function Assay 24/48 h induces G1 phase arrest in dose- and time dependent manner 25743822
A459 1/2/4 μM Function Assay 48 h decreases the levels of p-Akt 25743822
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.61mL

2.12mL

1.06mL

21.21mL

4.24mL

2.12mL
参考文献

[1]Curtin NJ, Hughes AN. Pemetrexed disodium, a novel antifolate with multiple targets. Lancet Oncol. 2001 May;2(5):298-306

[2]Shih C, Chen VJ, Gossett LS, Gates SB, MacKellar WC, Habeck LL, Shackelford KA, Mendelsohn LG, Soose DJ, Patel VF, Andis SL, Bewley JR, Rayl EA, Moroson BA, Beardsley GP, Kohler W, Ratnam M, Schultz RM. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23

[3]Hanauske AR, Chen V, Paoletti P, Niyikiza C. Pemetrexed disodium: a novel antifolate clinically active against multiple solid tumors. Oncologist. 2001;6(4):363-73