| Identification | Back Directory | [Name]
RX-3117 | [CAS]
865838-26-2 | [Synonyms]
TV1360
TV-1360
CS-1677
RX-3117
TV 1360
RX-3117 (TV-1360)
TV-1360;FLUOROCYCLOPENTENYLCYTOSINE
RX-3117; RX3117; RX 3117; TV-1360; TV1360; TV 1360; FLUOROCYCLOPENTENYLCYTOSINE
4-Amino-1-[(1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)-2-cyclopenten-1-yl]-2(1H)-pyrimidinone
2(1H)-Pyrimidinone, 4-amino-1-[(1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)-2-cyclopenten-1-yl]- | [Molecular Formula]
C10H12FN3O4 | [MDL Number]
MFCD28502078 | [MOL File]
865838-26-2.mol | [Molecular Weight]
257.22 |
| Chemical Properties | Back Directory | [Boiling point ]
516.3±60.0 °C(Predicted) | [density ]
1.82±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:50.0(Max Conc. mg/mL);194.39(Max Conc. mM) | [form ]
Powder | [pka]
12.88±0.70(Predicted) | [color ]
White to off-white | [InChI]
InChI=1S/C10H12FN3O4/c11-6-4(3-15)8(16)9(17)7(6)14-2-1-5(12)13-10(14)18/h1-2,7-9,15-17H,3H2,(H2,12,13,18)/t7-,8-,9+/m1/s1 | [InChIKey]
QLLGKCJUPWYJON-HLTSFMKQSA-N | [SMILES]
C1(=O)N([C@H]2[C@H](O)[C@H](O)C(CO)=C2F)C=CC(N)=N1 |
| Hazard Information | Back Directory | [Uses]
RX-3117 (TV-1360) is a potent and orally active anticancer and antimetaboliteagent. RX-3117 inhibits DNA methyltransferase 1 (DNMT1). RX-3117 shows antiproliferative and anti-tumour activity. RX-3117 induces cell cycle arrest at S phase and apoptosis[1][2][3]. | [Definition]
ChEBI:Roducitabine is a triol that is (1S,2R)-4-fluoro-3-(hydroxymethyl)cyclopent-3-ene-1,2-diol which is substituted by a 4-amino-2-oxopyrimidin-1(2H)-yl group at position 5. It is a cytidine analog which exhibits anticancer activity in several cancers, including gemcitabine-resistant tumours. It has a role as an antimetabolite, an antineoplastic agent, a prodrug, a DNA synthesis inhibitor and an apoptosis inducer. It is an organofluorine compound, a primary allylic alcohol and a triol. | [in vivo]
RX-3117 (2, 10 mg/kg; i.p.; three times per week for five weeks) shows anti-tumour activity in nude mice[3]. | Animal Model: | Nude mice (human colon carcinoma HCT116 xenograft model)[3] | | Dosage: | 2, 10 mg/kg | | Administration: | I.p.; three times per week for five weeks | | Result: | Caused significant inhibition of tumor growth at the doses of 2 and 10 mg/kg. |
| [storage]
Store at -20°C | [References]
[1] Sarkisjan D, et al. The Cytidine Analog Fluorocyclopentenylcytosine (RX-3117) Is Activated by Uridine-Cytidine Kinase 2. PLoS One. 2016 Sep 9;11(9):e0162901. DOI:10.1371/journal.pone.0162901
[2] Balboni B, et al. RX-3117 (fluorocyclopentenyl cytosine): a novel specific antimetabolite for selective cancer treatment. Expert Opin Investig Drugs. 2019 Apr;28(4):311-322. DOI:10.1080/13543784.2019.1583742
[3] Fahy J, et al. DNA methyltransferase inhibitors in cancer: a chemical and therapeutic patent overview and selected clinical studies. Expert Opin Ther Pat. 2012 Dec;22(12):1427-42. DOI:10.1517/13543776.2012.729579 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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