2. Cell Cycle/DNA Damage
  3. Topoisomerase
  4. TAS-103

TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.

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

TAS-103

TAS-103 Chemical Structure

CAS No. : 174634-08-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg 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

Other Forms of TAS-103:

TAS-103 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TAS-103

View All Topoisomerase Isoform Specific Products:

View All Isoforms
Topoisomerase Topo I Topo II DNA gyrase

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.

IC50 & Target[1]

Topoisomerase I

 

Topoisomerase II

 

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
0.033 μM
Compound: 1a, TAS-103
Cytotoxicity against human mitoxantrone-sensitive HL60 cells after 72 hrs
Cytotoxicity against human mitoxantrone-sensitive HL60 cells after 72 hrs
[PMID: 18507368]
HL60/MX2 IC50
2.7 μM
Compound: 1a, TAS-103
Cytotoxicity against mitoxantrone-resistant human HL60/MX2 cells after 72 hrs
Cytotoxicity against mitoxantrone-resistant human HL60/MX2 cells after 72 hrs
[PMID: 18507368]
KB IC50
0.0096 μM
Compound: TAS-103
Antiproliferative activity against human KB cells
Antiproliferative activity against human KB cells
[PMID: 34052677]
In Vitro

TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells[1]. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103[2]. TAS-103 inhibits the viability of HeLa cells, with an IC50 of 40 nM. TAS-103 (10 μM) disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation[3].

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

TAS-103 Related Antibodies
In Vivo

TAS-103 (30 mg/kg, i.v.) causes significant tumor growth suppression in mice bearing Lewis lung carcinoma (LLC) cells, without obvious body weight loss, and the liposomal TAS-103 is more active than free TAS-103[2].

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

333.38

Formula

C20H19N3O2
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C(C1=C2C3=CC=C(O)C=C3N=C1NCCN(C)C)C4=C2C=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 120 mg/mL (359.95 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 2.9996 mL 14.9979 mL 29.9958 mL
5 mM 0.5999 mL 2.9996 mL 5.9992 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (9.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3 mg/mL (9.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[1]

CCRF-CEM human acute lymphoblastic leukaemia cells are grown in RPMI-1640 supplemented with 3 mM l-glutamine, 10% foetal bovine serum, 50 U/mL of penicillin, and 40 μg/mL of streptomycin at 37°C in a humidified atmosphere containing 5% CO2. TAS-103, CPT and DACA are dissolved in DMSO. Exponentially growing cells (∼5 × 105) are exposed to either of the drugs for 2 hrs. Following drug exposure, cells are washed twice by centrifugation (400 × g, 3 min) in cold phosphate-buffered saline[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Lewislung carcinoma (LLC) cells are diluted with DMEM to obtain 5×106 cells/mL suspension, and 0.2 mL of the suspension is carefully injected subcutaneously into five-week-old C57BL/6 male mice. Liposomal TAS-103 (0.2 mL/mouse, 30 mg/kg as TAS-103), free TAS-103 or PBS is injected intravenously into a tail vein of the tumor-bearing mice on days 4, 8, and 12 after tumor implantation. Tumor volume of each mouse and the body weight change as an indicator of side effect are monitored daily thereafter. Tumor volume is calculated[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9996 mL 14.9979 mL 29.9958 mL 74.9895 mL
5 mM 0.5999 mL 2.9996 mL 5.9992 mL 14.9979 mL
10 mM 0.3000 mL 1.4998 mL 2.9996 mL 7.4990 mL
15 mM 0.2000 mL 0.9999 mL 1.9997 mL 4.9993 mL
20 mM 0.1500 mL 0.7499 mL 1.4998 mL 3.7495 mL
25 mM 0.1200 mL 0.5999 mL 1.1998 mL 2.9996 mL
30 mM 0.1000 mL 0.4999 mL 0.9999 mL 2.4997 mL
40 mM 0.0750 mL 0.3749 mL 0.7499 mL 1.8747 mL
50 mM 0.0600 mL 0.3000 mL 0.5999 mL 1.4998 mL
60 mM 0.0500 mL 0.2500 mL 0.4999 mL 1.2498 mL
80 mM 0.0375 mL 0.1875 mL 0.3749 mL 0.9374 mL
100 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7499 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.

TAS-103 Related Classifications

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.

Keywords:

TAS-103174634-08-3BMS-247615TAS103TAS 103BMS247615BMS 247615TopoisomeraseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
TAS-103
Cat. No.:
HY-13758
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.