Raltitrexed,112887-68-0

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YZ剂描述：

产品名称：Raltitrexed

产品别名：雷替曲塞

英文别名：ZD1694;D1694;ICI-D1694

靶点：Thymidylate Synthase

CAS：112887-68-0

纯度：>98%

外观：淡黄色或类白色粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Raltitrexed是一种胸苷酸合成酶YZ剂，YZL1210细胞生长，IC50为9 nM。

溶解性：DMSO ：84 mg/mL (183.2 mM)

体外研究：

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. 

体内研究：Raltitrexed could be directly transported into the brain via the olfactory pathway in rats.

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