A DNA topoisomerase I and II inhibitor
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TAS 103 (hydrochloride)

Item No. 29869

Technical Information
Formal Name
6-[[2-(dimethylamino)ethyl]amino]-3-hydroxy-7H-indeno[2,1-c]quinolin-7-one, dihydrochloride
CAS Number
174634-09-4
Molecular Formula
C20H19N3O2 • 2HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
PBS (pH 7.2): 1 mg/ml
λmax
229, 244, 262, 292 nm
SMILES
O=C1C(C(NCCN(C)C)=NC2=C3C=CC(O)=C2)=C3C4=C1C=CC=C4.Cl.Cl
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
InChi Key
HAYAYGFVSIWSGQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TAS 103 is an inhibitor of DNA topoisomerase I and II (IC50s = 2 and 6.5 µM, respectively).1 It stabilizes topoisomerase I-DNA and topoisomerase II-DNA cleavable complexes in KB cells when used at a concentration of 3 µM. It is cytotoxic to P388 and KB cells (IC50s = 1.1 and 9.6 nM, respectively). TAS 103 (15, 26, and 45 mg/kg per day) reduces pulmonary metastasis in murine B16-BL6 melanoma and UV-2237M fibrosarcoma models of lung metastasis. It also reduces tumor growth in a variety of human cancer mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Utsugi, T., Aoyagi, K., Asao, T., et alAntitumor activity of a novel quinoline derivative, TAS-103, with inhibitory effects on topoisomerases I and II. Jpn. J. Cancer Res. 88(10), 992-1002 (1997).