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首页 / 抑制剂/激动剂 / 细胞周期 / DHFR / Pemetrexed

培美曲塞 /Pemetrexed {[allProObj[0].p_purity_real_show]}

货号：A159122 同义名： 培美曲唑 / LY231514

Pemetrexed(LY231514) 是一种抗叶酸剂，其对胸苷酸合成酶 (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 值分别为 1.3 nM、7.2 nM 和 65 nM。

Pemetrexed 化学结构 CAS号：137281-23-3
Pemetrexed 化学结构
CAS号：137281-23-3
Pemetrexed 3D分子结构
CAS号：137281-23-3
Pemetrexed 化学结构 CAS号：137281-23-3
Pemetrexed 3D分子结构 CAS号：137281-23-3
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Pemetrexed 纯度/质量文件 产品仅供科研

货号：A159122 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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 生物活性

靶点

  • DHFR

    DHFR , Ki:7.2 nM
描述 The biologically active form of folic acid is tetrahydrofolate which is essential for DNA synthesis. Tetrahydrofolate is oxidised to dihydrofolate during DNA synthesis and is regenerated to its active form by the enzyme dihydrofolate reductase. Inhibition of this enzyme prevents DNA synthesis and causes failure of cell renewal. This leads to breaks in epithelial surfaces resulting in oropharyngeal and intestinal ulceration [5]. Pemetrexed is a new type of anti-folate and anti-metabolic drug, acting on TS, DHFR and GARFT, with Ki of 1.3nm, 7.2nm and 65nm in cell-free assay, respectively [6]. Pemetrexed is used in CCRF-CEM leukemia, GC3/C1 colon cancer, and HCT-8 cecum cancer cells with anti-proliferation activity with IC50 of 25 nM, 34 nM, and 220 nM, respectively. In addition, the combination of thorax and hypoxanthine on the above three cell lines completely reverses the cytotoxicity caused by pemetrexed [7]. SOCS-1 (suppressor of cytokine signaling 1, an endogenous inhibitor of intracellular signaling pathways) gene delivery cooperated with cisplatin plus pemetrexed to inhibit cell proliferation, invasiveness and induction of apoptosis in MPM cells [8]. Administration of the pemetrexed 6 h prior to administration of 5-fluorouracil resulted in additive growth delay of the MX-1 tumor. In addition, the simultaneous combination of MTA administered daily for 5 days for 2 weeks with administration of gemcitabine resulted in greater-than-additive H460 TGD [9].

Pemetrexed 动物研究

Dose Rat: 10 mg/kg, 100 mg/kg[3] (i.v.)
Administration i.v.
Pharmacokinetics
Animal Mice[4] Dogs
Dose 20 mg/kg 7.5 mg/kg
Administration i.v. or i.p. i.v.
AUC0→24h 33 μg·h/ml
t1/2α 5 - 20 min
Tmax 0.083 h (i.v.)
0.25 h (i.p.) 		5 min
T1/2β 7.0 h (i.v.)
7.8 h (i.p.)
Cmax 41 μg/ml (i.v.)
33 μg/ml (i.p.)
t1/2β 2.8 h
T1/2α 0083 - 0.5 h (i.v.)
AUC 31 μg·h/ml (i.v.)
44 μg·h/ml (i.p.)

Pemetrexed 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03655834 Non Small Cell Lung Cancer ... 展开 >> Mesothelioma 收起 << Phase 4 Not yet recruiting September 1, 2021 Netherlands ... 展开 >> Jeroen Bosch Hospital Not yet recruiting 's-Hertogenbosch, Netherlands Contact: Bonne Biesma       b.biesma@jbz.nl    Principal Investigator: Bonne Biesma          Sub-Investigator: Jeroen Derijks          Antoni van Leeuwenhoek Not yet recruiting Amsterdam, Netherlands Contact: Sjaak Burgers       s.burgers@nki.nl    Principal Investigator: Sjaak Burgers          Sub-Investigator: Alwin Huitema          Maastricht University Medical centre Not yet recruiting Maastricht, Netherlands Contact: Anne-Marie Dingemans       a.dingemans@mumc.nl    Principal Investigator: Anne-Marie Dingemans          Radboud university medical centre Not yet recruiting Nijmegen, Netherlands Contact: Rob ter Heine       R.terHeine@radboudumc.nl    Principal Investigator: Rob ter Heine          Sub-Investigator: Nikki de Rouw          Sub-Investigator: Michel van den Heuvel          Erasmus University Medical Centre Not yet recruiting Rotterdam, Netherlands Contact: Joachim Aerts       j.aerts@erasmusmc.nl    Principal Investigator: Joachim Aerts          Sub-Investigator: Ron Mathijsen 收起 <<
NCT02211833 Carcinoma, Non-Small-Cell Lung Phase 1 Completed - -
NCT02049060 Malignant Pleural Mesothelioma... 展开 >> Nonsquamous Nonsmall Cell Neoplasm of Lung 收起 << Phase 1 Phase 2 Active, not recruiting December 2017 Italy ... 展开 >> Istituto Clinico Humanitas Rozzano, Milan, Italy, 20089 收起 <<

Pemetrexed 参考文献

[1]Norris RE, Rappaport EF, Adamson PC. Preclinical evaluation of pemetrexed in pediatric solid tumors. Pediatr Blood Cancer. 2011 Dec 15;57(7):1233-5.

[2]Shih C, Chen VJ, 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.

[3]Sørensen JB, et al. Pharmacokinetic evaluation of pemetrexed. Expert Opin Drug Metab Toxicol. 2011 Jul;7(7):919-28.

[4]LY-231514

[5]Calcium leucovorin - folinic acid rescue. Drug Ther Bull. 1978 Feb 3;16(3):11-2.

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

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

[8]Iwahori K. SOCS-1 gene delivery cooperates with cisplatin plus pemetrexed to exhibit preclinical antitumor activity against malignant pleural mesothelioma. Int J Cancer. 2013 Jan 15;132(2):459-71. doi: 10.1002/ijc.27611. Epub 2012 May 17.

[9]Teicher BA. Treatment regimens including the multitargeted antifolate LY231514 in human tumor xenografts. Clin Cancer Res. 2000 Mar;6(3):1016-23.

Pemetrexed 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.70mL

2.34mL

1.17mL

23.40mL

4.68mL

2.34mL

Pemetrexed 技术信息

CAS号137281-23-3
分子式C20H21N5O6
分子量 427.411
别名 培美曲唑 ;LY231514
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C
溶解度

DMSO: 250 mg/mL(584.92 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
动物实验配方

Tags: Pemetrexed | LY231514 | 培美曲唑 | DHFR | AmBeed-信号通路专用抑制剂 | Pemetrexed 纯度/质量文件 | Pemetrexed 亚型比较 | Pemetrexed 生物活性 | Pemetrexed 动物研究 | Pemetrexed 临床数据 | Pemetrexed 参考文献 | Pemetrexed 实验方案 | Pemetrexed 技术信息

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