[CAS NO. 174634-09-4] TAS-103dihydrochloride

Name: TAS-103dihydrochloride
Brand: Arctom Scientific
SKU: AS023155

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PRODUCTS SPECIFICATIONS [174634-09-4]

Distributor

Catalog

AS023155

Brand

Arctom Scientific

CAS

174634-09-4

DESCRIPTION [174634-09-4]

Overview

MDL	MFCD00943251
Molecular Weight	406.31
Molecular Formula	C20H21Cl2N3O2
SMILES	O=C(C1=C2C3=CC=C(O)C=C3N=C1NCCN(C)C)C4=C2C=CC=C4.Cl.Cl

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

1 Publications Citing Use of MCE

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

Summary

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

IC50 & Target

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 IC ₅₀ 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 IC ₅₀ 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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H ₂ O : 5 mg/mL ( 12.31 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 3.57 mg/mL (8.79 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

* All of the co-solvents are available by MCE.

References

Synonyms

7H-Indeno[2,1-c]quinolin-7-one, 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-, hydrochloride (1:2)

7H-Indeno[2,1-c]quinolin-7-one, 6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-, dihydrochloride

6-[[2-(Dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one hydrochloride (1:2)

TAS 103