Name | RX-3117 |
Description | RX-3117 (fluorocyclopentenylcytosine) is a novel a cytidine analog. RX-3117 displays anticancer activity in several cancer cell lines, including gemcitabine-resistant variants. |
In vitro | 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]. |
In vivo | 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]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 50 mg/mL (194.39 mM)
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Keywords | TV1360 | TV 1360 | S phase | RX-3117 | RX3117 | RX 3117 | orally active | Nucleoside Antimetabolite/Analog | Inhibitor | inhibit | DNMT1 | apoptosis | anti-tumour | antiproliferative |
Inhibitors Related | Stavudine | 5-Fluorouracil | Floxuridine | Gemcitabine hydrochloride | 5-Azacytidine | Doxifluridine | 5-BrdU | Cytidine | Adenosine 5'-monophosphate disodium salt | Orotic acid | Ganciclovir | 6-Mercaptopurine |
Related Compound Libraries | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Anti-Viral Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |