Product Introduction
Bioactivity


英文名: RX-3117

描述: RX-3117 (fluorocyclopentenylcytosine) 是一种新型的胞苷类似物，在几种癌细胞系中显示出抗癌活性，包括对吉西他滨耐药的变体。

体外活性: RX-3117 was a very poor substrate for cytidine deaminase (66,000-fold less than gemcitabine). RX-3117 showed a different sensitivity profile compared to cyclopentenyl-cytosine and azacytidine, substrates for uridine-cytidine-kinase. Insensitive U937 cells 1 μM RX-3117 resulted in 90% inhibition of RNA synthesis but 100 μM RX-3117 was required in A2780 and CCRF-CEM cells. RX-3117 at IC50 values did not affect the integrity of RNA [1].

体内活性: RX-3117 (p.o.) was examined in 9 different human tumor xenograft models grown subcutaneously in athymic nude mice. In the Colo 205, H460, H69 and CaSki models, gemcitabine treatment resulted in 28%, 30%, 25% and 0% tumor growth inhibition (TGI), respectively. Whereas oral treatment with RX-3117 induced 100%, 78%, 62% and 66% TGI, respectively [2].

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

溶解度: DMSO : 50 mg/mL (194.39 mM)


关键字: Nucleoside Antimetabolite/Analog | S phase | DNMT1 | inhibit | orally active | RX 3117 | apoptosis | RX3117 | antiproliferative | RX-3117 | TV 1360 | Inhibitor | TV1360 | anti-tumour

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