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Technical Data
| Formula | C21H22N4O6S |
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| Molecular Weight | 458.49 | CAS No. | 112887-68-0 | |
| Solubility (25°C)* | In vitro | DMSO | 92 mg/mL (200.65 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | 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] |
Protocol (from reference)
References
Customer Product Validation
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Selleck's Raltitrexed has been cited by 14 publications
| 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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.