Pemetrexed
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Pemetrexed(也称为pemetrexed disodium)是一种新型的抗叶酸抗代谢物，它可以作用于涉及嘌呤和嘧啶合成的多种酶。Pemetrexed是抗叶酸物GARFYT抑制剂lometroxol的类似物，和lometroxol具有相似的化学结构。叶酸的pterine部分的吡嗪环和桥部分的苄基分别被吡咯环和亚甲基得到lometroxol。Pemetrexed对TS、DHFR、GARFT和AICARFT抑制性很强，但是在一系列的肿瘤，包括非小细胞肺癌、恶性间皮瘤、乳房癌、结直肠癌、子宫颈癌、头部和颈部和膀胱中抑制活性较弱。
参考文献：
[1]. Luis Paz-Ares, Susana Bezares, Jose M. Tabernero, Daniel Castellanos, and Hernan Cortes-Funes. Review of a promising new agent-pemetrexed disodium. Cancer 2003; 97(8 Suppl):2056-2063.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 471.37 |
| Cas No. | 150399-23-8 |
| Formula | C20H19N5Na2O6 |
| Synonyms | Pemetrexed disodium, LY-231514, Pemetrexed Na |
| Solubility | insoluble in EtOH; ≥15.68 mg/mL in DMSO with gentle warming and ultrasonic; ≥30.67 mg/mL in H2O |
| Chemical Name | disodium;(2S)-2-[[4-[2-(2-amino-4-oxo-1,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]amino]pentanedioate |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=CC=C1CCC2=CNC3=C2C(=O)N=C(N3)N)C(=O)NC(CCC(=O)[O-])C(=O)[O-].[Na+].[Na+] |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| Cell experiment:[1] | |
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Cell lines |
Human tumor cell lines, including CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma |
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Reaction Conditions |
0.0001 ~ 30 μM pemetrexed for 72 h incubation |
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Applications |
Pemetrexed exerted antiproliferative activity in all three cell lines. Thymidine (5 μM) only increased the IC50 of pemetrexed versus CCRF-CEM cells by 5.5-fold, GC3/C1 by 18.7-fold, and HCT-8 by 15-fold. Higher drug concentrations of pemetrexed required the combination of thymidine and hypoxanthine to protect these cells. |
| Animal experiment:[2] | |
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Animal models |
An intrathoracic murine model of malignant mesothelioma |
|
Dosage form |
100 mg/kg Administered intraperitoneally from days 4 ~ 8 |
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Applications |
The combination of pemetrexed and regulatory T cell (Treg) blockade showed synergistic antitumor effects in murine malignant mesothelioma, resulting in prolonged survival. This combination was associated with decreased tumor-infiltrating Tregs, increased IL-2 production, dendritic cell maturation, and increased CD3+CD8+IFN-γ+ tumor-infiltrating T cells when compared with mice treated with pemetrexed alone or Treg blockade alone. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Shih C, Chen VJ, Gossett LS, et al. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Research, 1997, 57(6): 1116-1123. 2. Anraku M, Tagawa T, Wu L, et al. Synergistic antitumor effects of regulatory T cell blockade combined with pemetrexed in murine malignant mesothelioma. Journal of Immunology, 2010, 185(2):956-966. |
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| 描述 | Pemetrexed是TS（Ki = 1.3 nM）、DHFR（Ki = 7.2 nM）和GARFT（Ki = 65 nM）的一种新型的抗叶酸物抗代谢物。 | |||||
| 靶点 | TS | DHFR | GARFT | |||
| IC50 | 1.3 nM (Ki) | 7.2 nM (Ki) | 65 nM (Ki) | |||
质量控制和MSDS
- 批次:
化学结构
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