Catalog No.S1192 Synonyms: ZD-1694
Molecular Weight(MW): 458.49
Raltitrexed is a thymidylate synthase inhibitor with an IC50 of 9 nM for the inhibition of L1210 cell growth.
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Fig. 1. Raltitrexed dose-response curve. HEK293 parental and MRP5 transfected cells were plated in a 96-well plate at a density of 4000 cells/well in complete DMEM (10% FBS, 1% Pencillin/streptomycin) and allowed to incubate for 24h at 37°C, 5% CO2. Raltirexed was added and the cells allowed to incubate for 72h. Total DNA present in each well was then quantified using Cyquant® cell proliferation assay. Results show Total DNA as % of the DMSO-only control wells. Experiment was done in triplicate.
Raltitrexed purchased from Selleck.
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|Description||Raltitrexed 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 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. 
|In vivo||Raltitrexed could be directly transported into the brain via the olfactory pathway in rats. |
-  Peters GJ, et al. Eur J Cancer, 2000, 36(7), 916-924.
-  Van Cutsem E, et al. Ann Oncol, 2002, 13(4), 513-522.
-  Aschele C, et al. Clin Cancer Res, 1998, 4(5), 1323-1330.
|In vitro||DMSO||91 mg/mL (198.47 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03053167||Recruiting||ColoRectal Cancer||China Medical University, China|The First Affiliated Hospital of Dalian Medical University|The Second Affiliated Hospital of Dalian Medical University|Liaoning Tumor Hospital & Institute|Shengjing Hospital|General Hospital of Shenyang Military Region||December 2016||Phase 2|
|NCT02965248||Recruiting||Locally Advanced Colorectal Cancer||Fudan University||November 2016||Phase 2|
|NCT02992886||Recruiting||Rectal Neoplasms Malignant||Chinese Academy of Medical Sciences||September 2016||Phase 2|
|NCT02618356||Not yet recruiting||Metastatic Colon Cancer||Fudan University||December 2015||Phase 2|
|NCT02562599||Recruiting||Nasopharyngeal Carcinoma||Hubei Cancer Hospital||August 2015||Phase 2|
|NCT02485548||Recruiting||Head and Neck Squamous Cell Cancer||Jiangsu Cancer Institute & Hospital|Wuxi Cancer Hospital|Changzhou Cancer Hospital|Nanjing Cancer Hospital|Northern Jiangsu Province Peoples Hospital|The Second Hospital of Nanjing Medical University|Nanjing BenQ Hospital||June 2015||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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