RX-3117
- Product Name
- RX-3117
- CAS No.
- 865838-26-2
- Chemical Name
- RX-3117
- Synonyms
- TV1360;CS-1677;TV-1360;TV 1360;RX-3117;Roducitabine;RX-3117 (TV-1360);RX-3117, 10 mM in DMSO;TV-1360;FLUOROCYCLOPENTENYLCYTOSINE;RX-3117; RX3117; RX 3117; TV-1360; TV1360; TV 1360; FLUOROCYCLOPENTENYLCYTOSINE
- CBNumber
- CB02628369
- Molecular Formula
- C10H12FN3O4
- Formula Weight
- 257.22
- MOL File
- 865838-26-2.mol
RX-3117 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-3947
- Product name
- RX-3117
- Purity
- 98.38%
- Packaging
- 5mg
- Price
- $420
- Updated
- 2021/12/16
- Product number
- CS-3947
- Product name
- RX-3117
- Purity
- 98.38%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- CS-3947
- Product name
- RX-3117
- Purity
- 98.38%
- Packaging
- 50mg
- Price
- $2520
- Updated
- 2021/12/16
- Product number
- CD31000518
- Product name
- RX-3117
- Purity
- 98+%
- Packaging
- 5mg
- Price
- $245
- Updated
- 2021/12/16
- Product number
- CD31000518
- Product name
- RX-3117
- Purity
- 98+%
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
RX-3117 Chemical Properties,Usage,Production
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
RX-3117 Preparation Products And Raw materials
Raw materials
Preparation Products
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