Raltitrexed

製品コードS1192 バッチS119204

印刷

化学情報

Chemical Structure Synonyms ZD-1694, ICI-D1694, D1694 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H22N4O6S
分子量 458.49 CAS No. 112887-68-0
Solubility (25°C)* 体外 DMSO 92 mg/mL (200.65 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 Raltitrexed (ZD-1694) is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.
in vitro 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. [1] 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. [2] Raltitrexed combined with SN-38 results in synergistic cytotoxicity at broad dose-effect ranges in human colon cancer cells. [3] 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. [4] 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. [5] Raltitrexed is 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. [6]
in vivo Raltitrexed could be directly transported into the brain via the olfactory pathway in rats. [4]

プロトコル(参考用のみ)

カスタマーフィードバック

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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：

A positive feedback circuit between RN7SK snRNA and m6A readers is essential for tumorigenesis [ Mol Ther, 2022, S1525-0016(22)00717-1] PubMed: 36566349
Threonine Cavities Are Targetable Motifs That Control Alpha-Synuclein Fibril Growth [ ACS Chem Neurosci, 2022, 13(17):2646-2657] PubMed: 36001084
The novel mechanism of Med12-mediated drug resistance in a TGFBR2-independent manner [ Biochem Biophys Res Commun, 2022, 610:1-7] PubMed: 35461070
Raltitrexed regulates proliferation and apoptosis of HGC-27 cells by upregulating RSK4 [ BMC Pharmacol Toxicol, 2022, 23(1):65] PubMed: 36031631
A modular master regulator landscape controls cancer transcriptional identity [ Cell, 2021, 184(2):334-351.e20] PubMed: 33434495
Structural Bases for the Synergistic Inhibition of Human Thymidylate Synthase and Ovarian Cancer Cell Growth by Drug Combinations [ Cancers (Basel), 2021, 13(9)2061] PubMed: 33923290
Microparticle-Assisted Precipitation Screening Method for Robust Drug Target Identification [ Anal Chem, 2020, 10.1021/acs.analchem.0c02756] PubMed: 32933243
A Peptidic Thymidylate-Synthase Inhibitor Loaded on Pegylated Liposomes Enhances the Antitumour Effect of Chemotherapy Drugs in Human Ovarian Cancer Cells [ Int J Mol Sci, 2020, 21(12):E4452] PubMed: 32585842
MYC predetermines the sensitivity of gastrointestinal cancer to antifolate drugs through regulating TYMS transcription. [ EBioMedicine, 2019, 48:289-300] PubMed: 31648989
A temperature-sensitive phase-change hydrogel of tamoxifen achieves the long-acting antitumor activation on breast cancer cells. [ Onco Targets Ther, 2019, 12:3919-3931] PubMed: 31213826

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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