RX-3117

Modify Date: 2024-01-10 20:12:14

RX-3117 Structure
RX-3117 structure
Common Name RX-3117
CAS Number 865838-26-2 Molecular Weight 257.218
Density 1.8±0.1 g/cm3 Boiling Point 516.3±60.0 °C at 760 mmHg
Molecular Formula C10H12FN3O4 Melting Point N/A
MSDS N/A Flash Point 266.1±32.9 °C

 Use of RX-3117


RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a cytidine analog; shows anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.IC50 value: 0.4- >30 nM (15 cancer cell lines) [1]Target: cytidine analogin vitro: RX-3117 showed a different sensitivity profile compared to cyclopentenyl-cytosine (CPEC) and azacytidine, substrates for uridine-cytidine-kinase (UCK).RX-3117 was a very poor substrate for cytidine deaminase (66,000-fold less than gemcitabine). In sensitive 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: Orally-administered RX-3117 was examined in 9 different human tumor xenograft models (colon, non-small cell lung, small cell lung, pancreatic, renal and cervical), 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].

 Names

Name RX-3117
Synonym More Synonyms

 RX-3117 Biological Activity

Description RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a cytidine analog; shows anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.IC50 value: 0.4- >30 nM (15 cancer cell lines) [1]Target: cytidine analogin vitro: RX-3117 showed a different sensitivity profile compared to cyclopentenyl-cytosine (CPEC) and azacytidine, substrates for uridine-cytidine-kinase (UCK).RX-3117 was a very poor substrate for cytidine deaminase (66,000-fold less than gemcitabine). In sensitive 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: Orally-administered RX-3117 was examined in 9 different human tumor xenograft models (colon, non-small cell lung, small cell lung, pancreatic, renal and cervical), 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].
Related Catalog
References

[1]. Peters GJ, et al. Metabolism, mechanism of action and sensitivity profile of fluorocyclopentenylcytosine (RX-3117; TV-1360). Invest New Drugs. 2013 Dec;31(6):1444-57.

[2]. Yang MY, et al. A novel cytidine analog, RX-3117, shows potent efficacy in xenograft models, even in tumors that are resistant to gemcitabine. Anticancer Res. 2014 Dec;34(12):6951-9.

 Chemical & Physical Properties

Density 1.8±0.1 g/cm3
Boiling Point 516.3±60.0 °C at 760 mmHg
Molecular Formula C10H12FN3O4
Molecular Weight 257.218
Flash Point 266.1±32.9 °C
Exact Mass 257.081177
LogP -0.72
Vapour Pressure 0.0±3.0 mmHg at 25°C
Index of Refraction 1.721

 Synonyms

2(1H)-Pyrimidinone, 4-amino-1-[(1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)-2-cyclopenten-1-yl]-
0Z4A82I0JO
MFCD28502078
4-Amino-1-[(1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)-2-cyclopenten-1-yl]-2(1H)-pyrimidinone
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