Amsacrine hydrochloride

SKU: orb1301460

Description

Amsacrine hydrochloride is a topoisomerase II inhibitor used in research for acute myelogenous leukemia. It is applied in both in vitro and in vivo studies to investigate mechanisms of cytotoxicity and chemotherapeutic efficacy against hematological cancers.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 54301-15-4
• MW: 429.92
• Purity: 99.92% (May vary between batches)
• Formula: C₂₁H₂₀ClN₃O₃S
• SMILES: Cl.COc1cc(NS(C)(=O)=O)ccc1Nc1c2ccccc2nc2ccccc12
• Target: Autophagy,Topoisomerase
• Solubility: DMSO:4.3 mg/mL (10 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.33 mM)

Bioactivity

• In Vivo:
  In animals treated with various doses of amsacrine (0.5-12 mg kg(-1)), significant increases in micronucleated polychromatic erythrocytes were observed at 9 and 12 mg kg(-1), with higher doses causing significant suppression of erythroblast proliferation. Amsacrine exhibits high incidences of clastogenicity and low incidences of aneugenicity.
• In Vitro:
  Amsacrine hydrochloride blocked HERG currents in HEK 293 cells and Xenopus oocytes in a concentration-dependent manner, with IC50 values of 209.4 nm and 2.0 microm, respectively. HERG channels were primarily blocked in the open and inactivated states, and no additional voltage dependence was observed. Amsacrine caused a negative shift in the voltage dependence of both activation (-7.6 mV) and inactivation (-7.6 mV). HERG current block by amsacrine was not frequency dependent. The S6 domain mutations Y652A and F656A attenuated (Y652A) or abolished (F656A, Y652A/F656A) HERG current blockade, indicating that amsacrine binding requires a common drug receptor within the pore-S6 region.
• Cell Research:
  Voltage-clamp measurements of Xenopus oocytes were performed in a solution containing (in mM): 5 KCl, 100 NaCl, 1.5. CaCl2, 2 MgCl2 and 10 HEPES (pH adjusted to 7.4 with NaOH). Current and voltage electrodes were filled with 3 m KCl solution. For whole-cell patch-clamp recordings from HEK 293 cells, electrodes were filled with the following solution (in mM): 130 K-aspartate, 5.0 MgCl2, 5 EGTA, 4 ATP, 10 HEPES (pH adjusted to 7.2 with KOH). The external solution for these experiments contained (in mM): 137 NaCl, 4.0 KCl, 1.0 MgCl2, 1.8 CaCl2, 10 HEPES, 10 glucose (pH adjusted to 7.4 with NaOH). Amsacrine was prepared as 10 mm stock solution in DMSO and stored at -20℃. On the day of experiments, aliquots of the stock solution were diluted to the desired concentrations with the bath solution. HERG current amplitudes (recorded from Xenopus oocytes) were not significantly altered upon application of 1% DMSO (v v^-1; maximum bath concentration) for 20 min. In addition, DMSO did not affect HERG channel currents recorded from HEK 293 cells at concentrations up to 0.3% (maximum bath concentration in this study: 0.1% DMSO).

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

Autophagy, Amsacrine, Amsacrine Hydrochloride, Amsacrine hydrochloride, acridinyl anisidide, acridinyl anisidide hydrochloride, acridinyl anisidide Hydrochloride, Inhibitor, inhibit, m-AMSA, m-AMSA Hydrochloride, m-AMSA hydrochloride, Topoisomerase

Compound Identifiers

PubChem CID

148673