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

TAS-103 (Synonyms: BMS-247615)

Cat. No.: HY-13758
Handling Instructions

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 Chemical Structure

TAS-103 Chemical Structure

CAS No. : 174634-08-3

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Description

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

IC50 & Target[1]

Topoisomerase I

 

Topoisomerase II

 

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].

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

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].

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

Molecular Weight

333.38

Formula

C₂₀H₁₉N₃O₂

CAS No.
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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
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TAS-103
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HY-13758
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