865838-26-2
865838-26-2 structure
- Name: RX-3117
- Chemical Name: RX-3117
- CAS Number: 865838-26-2
- Molecular Formula: C10H12FN3O4
- Molecular Weight: 257.218
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Nucleoside Antimetabolite/Analog
- Create Date: 2018-01-09 14:15:16
- Modify Date: 2024-01-10 20:12:14
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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].
| Name | RX-3117 |
|---|---|
| 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 |
| 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]. |
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| Related Catalog | |
| References |
| 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 |