TAS-103 dihydrochloride

SKU: orb1299933

Description

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) is a dual topoisomerase I and II inhibitor developed as an investigational anticancer agent. It has demonstrated antitumor activity in both cellular assays and in vivo models, supporting its use in cancer research, particularly for studying novel chemotherapeutic mechanisms.

Research Area

Molecular Biology

Key Properties

• CAS Number: 174634-09-4
• MW: 406.31
• Purity: 97.78%
• Formula: C₂₀H₂₁Cl₂N₃O₂
• SMILES: Cl.Cl.CN(C)CCNc1nc2cc(O)ccc2c2-c3ccccc3C(=O)c12
• Target: Topoisomerase
• Solubility: H2O:50 mg/mL (123.06 mM)

Bioactivity

• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Topo II, Topoisomerase, Topo I, TAS 103, TAS 103 dihydrochloride, TAS 103 Dihydrochloride, TAS103, TAS-103, TAS-103 (dihydrochloride), TAS103 dihydrochloride, TAS103 Dihydrochloride, TAS-103 Dihydrochloride, inhibit, Inhibitor, BMS 247615, BMS 247615 Dihydrochloride, BMS247615, BMS-247615, BMS247615 Dihydrochloride, BMS-247615 Dihydrochloride, BMS-247615 dihydrochloride

Compound Identifiers

PubChem CID

135413532