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培美曲塞二钠盐 /Pemetrexed disodium 99.9%

货号:A206176 同义名: 培美曲塞二钠 / LY231514 disodium Ambeed 开学季,买赠积分,赢豪礼

Pemetrexed disodium (LY231514 disodium) 是一种抗叶酸类药物,其五聚谷氨酸形式能抑制胸苷酸合成酶 (TS)、二氢叶酸还原酶 (DHFR) 和甘氨酰胺核糖核苷酸甲酰转移酶 (GARFT),Ki 值分别为 1.3、7.2 和 65 nM。

Pemetrexed disodium 化学结构 CAS号:150399-23-8
Pemetrexed disodium 化学结构
CAS号:150399-23-8
Pemetrexed disodium 3D分子结构
CAS号:150399-23-8
Pemetrexed disodium 化学结构 CAS号:150399-23-8
Pemetrexed disodium 3D分子结构 CAS号:150399-23-8
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Pemetrexed disodium 纯度/质量文件 产品仅供科研

货号:A206176 标准纯度: 99.9%
批次查询: 批次纯度:

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98%
SU056 +

YB-1, IC50: 1.73 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。
产品名称 DHFR 其他靶点 纯度
Pralatrexate 99%+
Pemetrexed disodium ++++

DHFR, Ki: 7.2 nM

99.9%
Pyrimethamine ++

DHFR, IC50: 15.4 nM

98% HPLC
Pemetrexed ++++

DHFR , Ki: 7.2 nM

99+%
Methotrexate +

hDHFR, IC50: 24 nM

99% (contain ~10%water)
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Pemetrexed disodium 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].

Pemetrexed disodium 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
A459 4μM Apoptosis Assay 48 h induces apoptosis 25743822

Pemetrexed disodium 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

Pemetrexed disodium 实验方案

计算器
存储液制备 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

Pemetrexed disodium 技术信息

CAS号150399-23-8
分子式C20H19N5Na2O6
分子量 471.374
别名 培美曲塞二钠 ;LY231514 disodium
运输蓝冰
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
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