TAS-103 (Synonyms: BMS-247615)

Cat. No.: HY-13758: FAQs
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TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (TAS-103 dihydrochloride) usually boasts enhanced water solubility and stability.

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

TAS-103 Chemical Structure

CAS No. : 174634-08-3

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Other In-stock Forms of TAS-103:

TAS-103 dihydrochloride

Other Forms of TAS-103:

TAS-103 dihydrochloride In-stock

1 Publications Citing Use of MCE TAS-103

•J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]

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Topoisomerase Topo I Topo II

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]

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.

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.

174634-08-3

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

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Padget K, et al. An investigation into the formation of N- [2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and 6-[2-(dimethylamino)ethylamino]- 3-hydroxy-7H-indeno[2, 1-C]quinolin-7-one dihydrochloride (TAS-103) stabilised DNA topoisomerase I and II [Content Brief]

[2]. Shimizu K, et al. Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent. Biol Pharm Bull. 2002 Oct;25(10):1385-7. [Content Brief]

[3]. Yoshida M, et al. A new mechanism of 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride (TAS-103) action discovered by target screening with drug-immobilized affinity beads. Mol Pharmacol. 2008 Mar;73(3):987-94. Epu [Content Brief]

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	[1]. Padget K, et al. An investigation into the formation of N- [2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and 6-[2-(dimethylamino)ethylamino]- 3-hydroxy-7H-indeno[2, 1-C]quinolin-7-one dihydrochloride (TAS-103) stabilised DNA topoisomerase I and II [Content Brief] [2]. Shimizu K, et al. Cancer chemotherapy by liposomal 6-[12-(dimethylamino)ethyl]aminol-3-hydroxy-7H-indeno[2,1-clquinolin-7-one dihydrochloride (TAS-103), a novel anti-cancer agent. Biol Pharm Bull. 2002 Oct;25(10):1385-7. [Content Brief] [3]. Yoshida M, et al. A new mechanism of 6-((2-(dimethylamino)ethyl)amino)-3-hydroxy-7H-indeno(2,1-c)quinolin-7-one dihydrochloride (TAS-103) action discovered by target screening with drug-immobilized affinity beads. Mol Pharmacol. 2008 Mar;73(3):987-94. Epu [Content Brief]

TAS-103 Related Classifications

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The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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

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