雷替曲塞 T6632

Product Introduction
Bioactivity


英文名: Raltitrexed

描述: Raltitrexed (D1694) 是一种抗代谢药物，通过抑制胸苷酸合成酶起作用，可用于化疗。

体外活性: Raltitrexed induces double-stranded DNA breaks in a concentration-dependent manner. In Lovo cells and LS174T cell lines containing wild-type p53, Raltitrexed increases the levels of the Bax protein up to 5-fold. In human colon cancer cells, Raltitrexed is actively absorbed into cells and is then rapidly and extensively metabolized into a series of polyglutamates, which results in the effective inhibition of thymidylate synthase. Raltitrexed is delivered to the brain very quickly and can be detected in all brain tissues within 5 minutes. In human colon cancer cells, the combination of Raltitrexed and SN-38 results in a synergistic cytotoxic effect within a range of concentrations. Raltitrexed is a specific folate-based inhibitor of thymidylate synthase. The effect on the activity of advanced rectal cancer is similar to fluorouracil (5-fluorouracil) plus leucovorin. Raltitrexed produces activity by rapid cell entry and glutamination. The glutaminated derivatives are more than 100 times more active than the parent compound. In the HCT-8 cell line, Raltitrexed results in an increase in intracellular phosphoribosyl pyrophosphate (PRPD) indicating that the cytotoxic effect of Raltitrexed in combination with 5-FU is due to increased nucleotide formation of 5-FU. Combinations of Raltitrexed and folinic acid (5FU-FA) show a combination of mode-dependent, synergistic inhibition of proliferation, which is determined by measuring the combination series. Raltitrexed combined with Vorinostat produced significant synergistic effects of cell cycle perturbation and S-phase arrest.

体内活性: Raltitrexed can be transported directly into the brain through the olfactory pathway in rats.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
5% DMSO+95% Saline : 4.2 mg/mL (9.16 mM, suspension)
DMSO : 84 mg/mL (183.2 mM)


关键字: Thymidylate Synthase | ICI-D-1694 | D-1694 | ZD-1694 | inhibit | D 1694 | Raltitrexed | Nucleoside Antimetabolite/Analog | Inhibitor | ICI-D 1694 | ZD 1694

相关产品: N6-Bz-5'-O-DMTr-3'-deoxyadenosine-2'-O-CED-phosphoramidite | Isoguanine | 2'-Deoxy-2'-fluorocytidine | 5-Azacytidine | Vidarabine | LY2334737 | Fludarabine | 2′-O-Methylcytidine | Dihydro-5-azacytidine acetate | Ganciclovir sodium

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Pediatric Drug Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途