Cat. No.: HY-15228

RX-3117

(Synonyms: TV-1360; Fluorocyclopentenylcytosine)

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.25%
CAS No.: 865838-26-2
Formula: C₁₀H₁₂FN₃O₄
Molecular Weight:257.22

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

RX-3117 Chemical Structure

CAS No.: 865838-26-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.5 μM Compound: 5a	Antitumor activity against human A549 cells by SRB method Antitumor activity against human A549 cells by SRB method	[PMID: 22524616]
HCT-116	IC₅₀	0.19 μM Compound: 5a	Antitumor activity against human HCT116 cells by SRB method Antitumor activity against human HCT116 cells by SRB method	[PMID: 22524616]
HeLa	IC₅₀	1.35 μM Compound: 5a	Antitumor activity against human HeLa cells by SRB method Antitumor activity against human HeLa cells by SRB method	[PMID: 22524616]
HepG2	IC₅₀	0.79 μM Compound: 5a	Antitumor activity against human HepG2 cells by SRB method Antitumor activity against human HepG2 cells by SRB method	[PMID: 22524616]
HT-29	IC₅₀	0.28 μM Compound: 5a	Antitumor activity against human HT-29 cells by SRB method Antitumor activity against human HT-29 cells by SRB method	[PMID: 22524616]
K562	IC₅₀	0.82 μM Compound: 5a	Antitumor activity against human K562 cells by SRB method Antitumor activity against human K562 cells by SRB method	[PMID: 22524616]
LNCaP	IC₅₀	2.67 μM Compound: 5a	Antitumor activity against human LNCAP cells by SRB method Antitumor activity against human LNCAP cells by SRB method	[PMID: 22524616]
MCF7	IC₅₀	0.34 μM Compound: 5a	Antitumor activity against human MCF7 cells by SRB method Antitumor activity against human MCF7 cells by SRB method	[PMID: 22524616]
MDA-MB-231	IC₅₀	0.18 μM Compound: 5a	Antitumor activity against human MDA-MB-231 cells by SRB method Antitumor activity against human MDA-MB-231 cells by SRB method	[PMID: 22524616]
MKN-45	IC₅₀	0.34 μM Compound: 5a	Antitumor activity against human MKN45 cells by SRB method Antitumor activity against human MKN45 cells by SRB method	[PMID: 22524616]
NCI-H226	IC₅₀	0.25 μM Compound: 5a	Antitumor activity against human NCI-H226 cells by SRB method Antitumor activity against human NCI-H226 cells by SRB method	[PMID: 22524616]
OVCAR-3	IC₅₀	0.8 μM Compound: 5a	Antitumor activity against human OVCAR3 cells by SRB method Antitumor activity against human OVCAR3 cells by SRB method	[PMID: 22524616]
PANC-1	IC₅₀	0.62 μM Compound: 5a	Antitumor activity against human PANC1 cells by SRB method Antitumor activity against human PANC1 cells by SRB method	[PMID: 22524616]
PC-3	IC₅₀	0.63 μM Compound: 5a	Antitumor activity against human PC3 cells by SRB method Antitumor activity against human PC3 cells by SRB method	[PMID: 22524616]
SK-MEL-28	IC₅₀	1.38 μM Compound: 5a	Antitumor activity against human SK-MEL-28 cells by SRB method Antitumor activity against human SK-MEL-28 cells by SRB method	[PMID: 22524616]
U-251	IC₅₀	0.83 μM Compound: 5a	Antitumor activity against human U251 cells by SRB method Antitumor activity against human U251 cells by SRB method	[PMID: 22524616]

In Vitro

RX-3117 causes both inhibition of DNA and RNA synthesis^[1].
RX-3117 (11.7, 21 μM; 48 h) shows antiproliferative activity in A549, SW1573 cells^[1].
RX-3117 is activated by uridine-cytidine kinase 2 (UCK2)^[1].
RX-3117 (1-25 μM; 72 h) inhibits the growth of HCT-116, MDA-MB-231, PANC-1, Caki-1, MCF7, A549, MKN45, U251 cells with IC₅₀s of 0.39, 0.18, 0.62, 0.84, 0.34, 0.34, 0.50, 0.83 μM, respectively^[2].
RX-3117 (5, 10 μM; 4 days) induces cell cycle arrest at S phase and apoptosis^[2].
RX-3117 (1-5 μM; 24 h) decreases the cellular amount of DNMT1 in a dose-dependent manner in MDA-MB-231^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

A549, SW1573 cells
Concentration:

11.7, 21 µM
Incubation Time:

48 h
Result:

Showed antiproliferative activity in A549 (63.7% cell growth), SW1573 cells (59% cell growth).

Apoptosis Analysis^[2]

Cell Line:

A549, SW1573 NSCLC cells
Concentration:

5 µM for A549 cells, 10 µM for SW1573 cells
Incubation Time:

4 days
Result:

Induced cell cycle arrest at S phase and apoptosis.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 865838-26-2
Appearance Solid
Molecular Weight 257.22
Formula C₁₀H₁₂FN₃O₄
Color White to off-white
SMILES

O=C1N([C@@H]2C(F)=C(CO)[C@@H](O)[C@H]2O)C=CC(N)=N1
Synonyms

TV-1360; Fluorocyclopentenylcytosine
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Patent

US20250102493A1.
bioRxiv

Oncogene-like addiction to aneuploidy in human cancers. [Abstract]

2023 Jan 10:2023.01.09.523344. PMID: 36711674

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (194.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.8877 mL

19.4386 mL

38.8772 mL

5 mM

0.7775 mL

3.8877 mL

7.7754 mL

10 mM

0.3888 mL

1.9439 mL

3.8877 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.8877 mL	19.4386 mL	38.8772 mL	97.1931 mL
	5 mM	0.7775 mL	3.8877 mL	7.7754 mL	19.4386 mL
	10 mM	0.3888 mL	1.9439 mL	3.8877 mL	9.7193 mL
	15 mM	0.2592 mL	1.2959 mL	2.5918 mL	6.4795 mL
	20 mM	0.1944 mL	0.9719 mL	1.9439 mL	4.8597 mL
	25 mM	0.1555 mL	0.7775 mL	1.5551 mL	3.8877 mL
	30 mM	0.1296 mL	0.6480 mL	1.2959 mL	3.2398 mL
	40 mM	0.0972 mL	0.4860 mL	0.9719 mL	2.4298 mL
	50 mM	0.0778 mL	0.3888 mL	0.7775 mL	1.9439 mL
	60 mM	0.0648 mL	0.3240 mL	0.6480 mL	1.6199 mL
	80 mM	0.0486 mL	0.2430 mL	0.4860 mL	1.2149 mL
	100 mM	0.0389 mL	0.1944 mL	0.3888 mL	0.9719 mL

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RX-3117

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) RX-3117

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RX-3117

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) RX-3117

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RX-3117 Related Classifications

HY-15228 Related Classifications