Pemetrexed

製品コードS5971 バッチS597102

印刷

化学情報

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	10.000mg/ml (23.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.

参考

https://pubmed.ncbi.nlm.nih.gov/9067281/
https://pubmed.ncbi.nlm.nih.gov/22532243/
https://pubmed.ncbi.nlm.nih.gov/10741729/

https://pubmed.ncbi.nlm.nih.gov/35093869/

+ 展开

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：

EXO1 as a therapeutic target for Fanconi Anaemia, ZRSR2 and BRCA1-A complex deficient cancers [ Nat Commun, 2025, 16(1):8476]	PubMed: 41006228
WWC proteins-mediated compensatory mechanism restricts schwannomatosis driven by NF2 loss of function [ Sci Adv, 2025, 11(4):eadp4765]	PubMed: 39841844
AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients With MTAP-Deleted Cancers [ Cancer Discov, 2024, 10.1158/2159-8290.CD-24-0887]	PubMed: 39282709
Neoadjuvant sintilimab plus chemotherapy in EGFR-mutant NSCLC: Phase 2 trial interim results (NEOTIDE/CTONG2104) [ Cell Rep Med, 2024, 5(7):101615]	PubMed: 38897205
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
Protocol for generation of and high-throughput drug testing with patient-derived colorectal cancer organoids [ STAR Protoc, 2024, 5(2):103090]	PubMed: 38809757
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

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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