Pemetrexed

製品コードS5971 バッチS597103

印刷

化学情報

Chemical Structure Synonyms LY231514 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C20H21N5O6
分子量 427.41 CAS No. 137281-23-3
Solubility (25°C)* 体外 DMSO 85 mg/mL (198.87 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Pemetrexed (LY231514) is a novel antifolate and antimetabolite for thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase (GARFT) with Ki of 1.3 nM, 7.2 nM and 65 nM in cell-free assays, respectively. Pemetrexed induces autophagy and apoptosis.
in vitro

Osimertinib+pemetrexed treatment delays the emergence of resistance relative to monotherapy in vitro, also down-regulates the expression of the anti-apoptotic gene PLK1 in PC-9 and H1975.[4]
in vivo

The combination of omepetinib and pemetrexed enhances apoptosis via a PLK1 signaling pathway, and the anti-tumor effect against xenografts harboring the EGFR mutation in vivo.[4]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 PC-9 and NCI-H1975 (H1975) cells
濃度 0.001, 0.01, 0.1, 1, 10 μM
反応時間 72 h
実験の流れ

Cells are plated in 96-well tissue culture plates at 5,000 cells/well and incubated at 37 ℃ for 24 h. Cells are then incubated with titrated concentrations of the drugs (0.001, 0.01, 0.1, 1, 10 μM) or vehicle (DMSO) at 37 ℃ for 72 h. Cell numbers are estimated using the Counting Kit-8. Protein extraction and western blotting are performed. Apoptosis assays are performed using the Annexin V-FITC Apoptosis Detection Kit.
動物実験 動物モデル Female severe combined immunodeficient (SCID)-Beige mice injected with PC-9 cells
投薬量 100 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Metabolic Hallmarks for Purine Nucleotide Biosynthesis in Small Cell Lung Carcinoma [ Mol Cancer Res, 2024, 22(1):82-93] PubMed: 37773022
A novel lncRNA-hidden polypeptide regulates malignant phenotypes and pemetrexed sensitivity in A549 pulmonary adenocarcinoma cells [ Amino Acids, 2024, 56(1):15] PubMed: 38351332
Crosstalk with lung fibroblasts shapes the growth and therapeutic response of mesothelioma cells [ Cell Death Dis, 2023, 10.1038/s41419-023-06240-x] PubMed: 37938546
Exploring the Molecular Players behind the Potentiation of Chemotherapy Effects by Durvalumab in Lung Adenocarcinoma Cell Lines [ Pharmaceutics, 2023, 15(5)1485] PubMed: 37242727
Exploring the Molecular Players behind the Potentiation of Chemotherapy Effects by Durvalumab in Lung Adenocarcinoma Cell Lines [ Pharmaceutics, 2023, 15(5)1485] PubMed: 37242727
Gastrodin destabilizes survivin and overcomes pemetrexed resistance [ Cell Signal, 2023, 110:110851] PubMed: 37586466
SETD4 Confers Cancer Stem Cell Chemoresistance in Nonsmall Cell Lung Cancer Patients via the Epigenetic Regulation of Cellular Quiescence [ Stem Cells Int, 2023, 2023:7367854] PubMed: 37274024
Immunofluorescence-Based Assay for High-Throughput Analysis of Multidrug Resistance Markers in Non-Small Cell Lung Carcinoma Patient-Derived Cells [ Diagnostics (Basel), 2023, 13(24)3617] PubMed: 38132201
Immune checkpoint inhibitors modulate the cytotoxic effect of chemotherapy in lung adenocarcinoma cells [ Oncology Letters, 2023, 152] PubMed: None
Immune checkpoint inhibitors modulate the cytotoxic effect of chemotherapy in lung adenocarcinoma cells [ Oncol Lett, 2023, 25(4):152] PubMed: 36936028

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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