产品说明书
Pemetrexed
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同义名 : | 培美曲唑 ;LY231514 |
| CAS号 : | 137281-23-3 | |
| 货号 : | A159122 | |
| 分子式 : | C20H21N5O6 | |
| 纯度 : | 99+% | |
| 分子量 : | 427.411 | |
| MDL号 : | MFCD19105065 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 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]. | ||
| 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 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.34mL 0.47mL 0.23mL |
11.70mL 2.34mL 1.17mL |
23.40mL 4.68mL 2.34mL |
| 参考文献 |
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[5]Calcium leucovorin - folinic acid rescue. Drug Ther Bull. 1978 Feb 3;16(3):11-2. |