ChemicalBook Product Catalog Biochemical Engineering Biochemical Reagents Agonist Inhibitors RX-3117

RX-3117

Product NameRX-3117
CAS865838-26-2
MFC10H12FN3O4
MW257.22
EINECS
MOL File865838-26-2.mol

Chemical Properties

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)
pka	12.88±0.70(Predicted)
form	Powder
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

Usage And Synthesis

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.

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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