| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R408572-1ml |
1ml |
现货  |
|
| 英文别名 | ZD-1694 | N-[[5-[[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]methylamino]-2-thienyl]carbonyl]- L-glutamic acid |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Raltitrexed |
| 生化机理 | 雷替曲塞（ZD-1694）是一种胸苷酸合成酶抑制剂，抑制 L1210 细胞生长的 IC50 值为 9 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 胸腺嘧啶酸合成酶抑制剂 |
| 产品介绍 |
Raltitrexed是一种胸苷酸合成酶抑制剂，抑制L1210细胞生长，IC50为9 nM。An inhibitor of thymidylate synthase and DHFR. Information Raltitrexed Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth. Raltitrexed induces a concentration-dependent amount of double-stranded DNA breaks. Raltitrexed increases the level of Bax protein up to a factor 5 in the Lovo and LS174T cell lines containing wt p53. Raltitrexed leads to an increase of intracellular phosphoribosyl pyrophosphate (PRPD) in the case of the HCT-8 cell line, which suggests that the cytotoxic effects of raltitrexed combined with 5-FU may be due to the increased formation of 5-FU nucleotides. Raltitrexed combined with SN-38 results in synergistic cytotoxicity at broad dose-effect ranges in human colon cancer cells. Raltitrexed is actively taken up into cells and then undergoes rapid, extensive metabolism to a series of polyglutamates, which results in potent thymidylate synthase inhibition. Raltitrexed is delivered to the brain very quickly, and could be detected at 5 min in all brain tissues. Raltitrexed combined folinic acid (5FU-FA) shows a clear schedule-dependent synergistic antiproliferative interaction as demonstrated by calculating combination indexes. Raltitrexed combined with Vorinostat produces synergistic effect paralleled by evident cell cycle perturbations with major S-phase arrest. Raltitrexed\xa0is a specific, folate-based inhibitor of thymidylate synthase with activity in advanced colorectal cancer comparable with that of fluorouracil (5-fluorouracil) plus folinic acid. Raltitrexed‘s activity is enhanced by rapid cellular entry and polyglutamation, with the polyglutamated derivatives having approximately 100-fold greater inhibitory potency than the parent compound.\xa0 In vivo Raltitrexed could be directly transported into the brain via the olfactory pathway in rats. cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CN(CC1=CC2=C(C=C1)N=C(C)NC2=O)C3=CC=C(S3)C(=O)NC(CCC(O)=O)C(O)=O |
| 分子量 | 458.49 |
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
| 1. Yisheng Peng, Hui Liu, Xiaoliu Liang, Lei Cao, Minglei Teng, Hu Chen, Zhenjie Li, Xuqi Peng, Jingsong Mao, Hongwei Cheng, Gang Liu. (2025) Self-assembling chemodrug fiber-hydrogel for transarterial chemoembolization and radiotherapy-enhanced antitumor immunity. JOURNAL OF CONTROLLED RELEASE, 380 (1). [PMID:39892652] [10.1016/j.jconrel.2025.01.088] |
| 1. Yisheng Peng, Hui Liu, Xiaoliu Liang, Lei Cao, Minglei Teng, Hu Chen, Zhenjie Li, Xuqi Peng, Jingsong Mao, Hongwei Cheng, Gang Liu. (2025) Self-assembling chemodrug fiber-hydrogel for transarterial chemoembolization and radiotherapy-enhanced antitumor immunity. JOURNAL OF CONTROLLED RELEASE, 380 (1). [PMID:39892652] [10.1016/j.jconrel.2025.01.088] |
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