TAS-103 dihydrochloride

Alias: TAS103 diHCl; TAS-103 dihydrochloride; TAS 103 dihydrochloride; BMS247615diHCl; BMS 247615 diHCl; BMS-247615diHCl;BMS247615 dihydrochloride; BMS 247615 dihydrochloride; BMS-247615 dihydrochloride

Cat No.:V2860 Purity: ≥98%

COA Product Data Instructions for use SDS

TAS-103 dihydrochloride (also known as BMS-247615) is a potent and dual inhibitor of DNA topoisomerase I/II.

TAS-103 dihydrochloride Chemical Structure CAS No.: 174634-09-4
Product category: Topoisomerase

This product is for research use only, not for human use. We do not sell to patients.

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Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

TAS-103 dihydrochloride (also known as BMS-247615) is a potent and dual inhibitor of DNA topoisomerase I/II. In tumor models from mice and humans, this derivative of quinoline exhibits antitumor activity. TAS-103 has an IC50 value of 5 nM and is active on CCRF-CEM cells. In individual CCRF-CEM cells, TAS-103 at 0.1 μM significantly increases levels of topo IIα FITC immunofluorescence. HeLa cell viability is inhibited by TAS-103, with an IC50 of 40 nM. At 10 μM, TAS-103 prevents the formation of signal recognition particle (SRP) complexes and causes SRP14 and SRP19 to become unstable, leading to their eventual degradation. Despite the fact that TAS-103 has been described as a strong topoisomerase II poison. Nonetheless, alternative research has demonstrated that there is no association between topoisomerase II expression and cellular susceptibility to TAS-103.

Biological Activity I Assay Protocols (From Reference)

Targets

Topoisomerase II; Topoisomerase I

ln Vitro

TAS-103 is a DNA topoisomerase I/II dual inhibitor. TAS-103 exhibits activity on CCRF-CEM cells at concentrations 0.1-10 μM, with an IC50 of 5 nM. Individual CCRF-CEM cells exhibit significantly higher levels of topo IIα FITC immunofluorescence when exposed to TAS-103 (0.1 μM)[1]. Lewis lung carcinoma (LLC) cells are highly susceptible to TAS-103 (0.01-1 μM) cytotoxicity, and liposomal TAS-103 is nearly twice as active as free TAS-103[2]. HeLa cell viability is inhibited by TAS-103, with an IC50 of 40 nM. Signal recognition particle (SRP) complex formation is disrupted by TAS-103 (10 μM), which also causes SRP14 and SRP19 to become unstable and eventually degrade[3].

ln Vivo

TAS-103 (30 mg/kg, i.v.) significantly suppresses tumor growth in mice harboring Lewis lung carcinoma (LLC) cells, without obvious body weight loss. Additionally, liposomal TAS-103 exhibits higher activity than free TAS-103[2].

Cell Assay

Human acute lymphoblastic leukemia cells, designated as CCRF-CEM cells, are cultured in RPMI-1640 medium supplemented with 3 mM l-glutamine, 10% foetal bovine serum, 50 U/mL penicillin, and 40 μg/mL streptomycin. The culture is maintained at 37°C in a humidified environment with 5% CO₂. In DMSO, TAS-103, CPT, and DACA are dissolved. Both drugs are applied to exponentially growing cells (approximately 5 × 10⁵) for a duration of 2 hours. After being exposed to drugs, cells are centrifuged twice for three minutes at 400 × g in cold phosphate-buffered saline[1].

Animal Protocol

Male C57BL/6 mice, aged five weeks, receive a subcutaneous injection of 0.2 mL of a suspension containing 5×10⁶ cells/mL of diluted Lewislung carcinoma (LLC) cells, made using DMEM. The tumor-bearing mice are given intravenous injections of liposomal TAS-103 (0.2 mL/mouse, 30 mg/kg as TAS-103), free TAS-103, or PBS on days 4, 8, and 12 following tumor implantation. Every day after that, the tumor volume in each mouse is tracked, along with any changes in body weight that may indicate a side effect. One computes the tumor volume [2].

References

[1]. 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 cleavable complexes in human leukaemia cells. Biochem Pharmacol. 2000 Sep 15;60(6):817-21.

[3]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C20H21CL2N3O2

Molecular Weight

406.31

Exact Mass

405.1

Elemental Analysis

C, 59.12; H, 5.21; Cl, 17.45; N, 10.34; O, 7.88

CAS #

174634-09-4

Related CAS #

174634-08-3; 174634-09-4 (HCl salt)

Appearance

Red solid powder

SMILES

CN(C)CCNC1=NC2=C(C=CC(=C2)O)C3=C1C(=O)C4=CC=CC=C43.Cl.Cl

InChi Key

HAYAYGFVSIWSGQ-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H19N3O2.2ClH/c1-23(2)10-9-21-20-18-17(13-5-3-4-6-14(13)19(18)25)15-8-7-12(24)11-16(15)22-20;;/h3-8,11,24H,9-10H2,1-2H3,(H,21,22);2*1H

Chemical Name

6-[2-(dimethylamino)ethylamino]-3-hydroxyindeno[2,1-c]quinolin-7-one;dihydrochloride

Synonyms

TAS103 diHCl; TAS-103 dihydrochloride; TAS 103 dihydrochloride; BMS247615diHCl; BMS 247615 diHCl; BMS-247615diHCl;BMS247615 dihydrochloride; BMS 247615 dihydrochloride; BMS-247615 dihydrochloride

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: >10 mM

Water: >15 mg/mL

Ethanol: N/A

Solubility (In Vivo)

Solubility in Formulation 1: 3.57 mg/mL (8.79 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4612 mL	12.3059 mL	24.6117 mL
	5 mM	0.4922 mL	2.4612 mL	4.9223 mL
	10 mM	0.2461 mL	1.2306 mL	2.4612 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

Structures of the chemical compounds and preparation of TAS-1-3383-fixed latex beads.Mol Pharmacol.2008 Mar;73(3):987-94.
Affinity purification using TAS-1-3383-fixed beads.Mol Pharmacol.2008 Mar;73(3):987-94.
Effects of TAS-103 on the interactions between SRP54 and other subunits.Mol Pharmacol.2008 Mar;73(3):987-94.
Effects of TAS-103 on the SRP complex.Mol Pharmacol.2008 Mar;73(3):987-94.
Effects of TAS-103 and knockdowns of SRP14 or SRP54 on the translocation of IL-6-FLAG.Mol Pharmacol.2008 Mar;73(3):987-94.