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Synonyms | ZD-1694, ICI-D1694, D1694 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H22N4O6S |
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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. |
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. |
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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] |
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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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。