1. Cell Cycle/DNA Damage Apoptosis
  2. Nucleoside Antimetabolite/Analog Apoptosis
  3. RX-3117

RX-3117  (Synonyms: TV-1360; Fluorocyclopentenylcytosine)

Cat. No.: HY-15228 Purity: 98.38%
COA Handling Instructions

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.

RX-3117 Chemical Structure

RX-3117 Chemical Structure

CAS No. : 865838-26-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 566 In-stock
Solution
10 mM * 1 mL in DMSO USD 566 In-stock
Solid
1 mg USD 200 In-stock
5 mg USD 420 In-stock
10 mg USD 600 In-stock
50 mg USD 2520 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE RX-3117

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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
Molecular Weight

257.22

Formula

C10H12FN3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

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
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8877 mL 19.4386 mL 38.8772 mL
5 mM 0.7775 mL 3.8877 mL 7.7754 mL
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
RX-3117
Cat. No.:
HY-15228
Quantity:
MCE Japan Authorized Agent: