TAS-103 (dihydrochloride)

SKU: orb1220521

Description

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

Key Properties

• CAS Number: 174634-09-4
• MW: 406.31
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₁Cl₂N₃O₂
• SMILES: Cl.Cl.CN(C)CCNc1nc2cc(O)ccc2c2-c3ccccc3C(=O)c12
• Target: Topoisomerase
• Solubility: H2O:50 mg/mL (123.06 mM; Need ultrasonic)

Bioactivity

• 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.
• 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 IC50 value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells. 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. TAS-103 inhibits the viability of HeLa cells, with an IC50 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BMS-247615 dihydrochloride

Quick Database Links

Gene Symbol

Topoisomerase