RX-3117

SKU: orb1307765

Description

RX-3117 is a novel fluorocyclopentenylcytosine analog with demonstrated anticancer activity in vitro against various cancer cell lines, including those resistant to gemcitabine. Research applications include investigating its mechanism and efficacy in preclinical in vivo models for oncology.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 865838-26-2
• MW: 257.22
• Purity: 99.55% (May vary between batches)
• Formula: C₁₀H₁₂FN₃O₄
• SMILES: Nc1ccn([C@H]2[C@H](O)[C@H](O)C(CO)=C2F)c(=O)n1
• Target: Nucleoside Antimetabolite/Analog
• Solubility: DMSO:50 mg/mL (194.39 mM)

Bioactivity

• 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 .
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TV1360, TV-1360, TV 1360, RX 3117, RX3117, RX-3117, S phase, DNMT1, apoptosis, antiproliferative, anti-tumour, Analog, fluorocyclopentenylcytosine, Inhibitor, inhibit, NucleosideAntimetabolite, Nucleoside Antimetabolite/Analog, Nucleoside Antimetabolite, orally active

Compound Identifiers

PubChem CID

11242315