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TAS-103 dihydrochloride

Catalog No. T7309 CAS 174634-09-4

Synonyms: TAS-103 (dihydrochloride), BMS-247615 dihydrochloride

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) is a novel anticancer agent targeting both topoisomerase (Topo) I and Topo II.

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TAS-103 dihydrochloride Chemical Structure

TAS-103 dihydrochloride, CAS 174634-09-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 288.00
50 mg	In stock	$ 428.00
100 mg	In stock	$ 639.00

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Biological Description

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Storage & Solubility Information

Description

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) is a novel anticancer agent targeting both topoisomerase (Topo) I and Topo II.

In vitro

The in vitro antitumor effects of TAS-103 were compared with those of other known Topo I and Topo II inhibitors. TAS-103 inhibited DNA synthesis more strongly than RNA and protein synthesis, and induced an increase of cell population in the S-G2/M phase. The cytotoxicity of TAS-103 was strongest against S-phase cells, but its cell cycle phase specificity was not clear, and depended on drug concentration and exposure time. The cytotoxicity of TAS-103 (IC50: 0.0030-0.23 microM) against various tumor cell lines was much stronger than that of VP-16 and comparable to that of SN-38. The cytotoxicity of TAS-103 seemed to be more related to the amount of protein-DNA complexes than to the accumulation of TAS-103 in the cells. P-Glycoprotein (P-gp)-mediated MDR, CDDP-resistant and 5-FU-resistant cell lines did not show cross-resistance to TAS-103. Although PC-7/CPT cells bearing a Topo I gene mutation showed cross-resistance to TAS-103, the sensitivity of P388/CPT, HT-29/CPT and St-4/CPT cells, showing decreased Topo I expression, was not changed. KB/VM4 and HT-29/Etp cells, showing decreased Topo II expression, were slightly cross-resistant to TAS-103. These results suggest that TAS-103 may act as an inhibitor of both Topo I and Topo II at the cellular level[1].

Synonyms	TAS-103 (dihydrochloride), BMS-247615 dihydrochloride
Molecular Weight	406.31
Formula	C20H21Cl2N3O2
CAS No.	174634-09-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 50 mg/mL (123.06 mM), Sonication is recommended.

References and Literature

1. Aoyagi Y , Kobunai T , Utsugi T , et al. In vitro Antitumor Activity of TAS-103, a Novel Quinoline Derivative That Targets Topoisomerases I and II[J]. Japanese journal of cancer research: Gann, 1999, 90(5):578-587. 2. Ishida K , Asao T . Self-association and unique DNA binding properties of the anti-cancer agent TAS-103, a dual inhibitor of topoisomerases I and II[J]. Biochimica et Biophysica Acta, 2002, 1587(2-3):155-163.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Bioactive Compounds Library Max Bioactive Compound Library NO PAINS Compound Library Anti-Cancer Compound Library ReFRAME Related Library Anti-Aging Compound Library DNA Damage & Repair Compound Library

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Keywords

TAS-103 dihydrochloride 174634-09-4 DNA Damage/DNA Repair Topoisomerase TAS-103 TAS 103 inhibit TAS 103 dihydrochloride TAS-103 Dihydrochloride TAS-103 (dihydrochloride) Inhibitor TAS103 dihydrochloride BMS-247615 Dihydrochloride TAS103 Dihydrochloride TAS103 BMS-247615 BMS 247615 BMS-247615 dihydrochloride BMS 247615 Dihydrochloride TAS 103 Dihydrochloride BMS247615 BMS247615 Dihydrochloride inhibitor

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