Amsacrine

SKU: orb1309417

Description

Amsacrine (AMSA) is an antineoplastic agent that functions as a DNA intercalator and a topoisomerase II inhibitor. It is widely used in cancer research, particularly in studies of leukemia, for both in vitro cytotoxicity assays and in vivo tumor model experiments.

Research Area

Cell Biology, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 51264-14-3
• MW: 393.46
• Purity: >99.99% (May vary between batches)
• Formula: C₂₁H₁₉N₃O₃S
• SMILES: N(C=1C2=C(N=C3C1C=CC=C3)C=CC=C2)C4=C(OC)C=C(NS(C)(=O)=O)C=C4
• Target: Topoisomerase,Potassium Channel,Autophagy
• Solubility: DMSO:50 mg/mL (127.08 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.08 mM)

Bioactivity

• In Vivo:
  In animals treated with amsacrine (0.5-12 mg/kg), the frequencies of micronucleated polychromatic erythrocytes significantly increase at doses of 9 and 12 mg/kg. This study demonstrates for the first time that amsacrine exhibits high clastogenicity and low aneugenicity, while nocodazole exhibits high aneugenicity and low clastogenicity during mitotic phases in vivo.
• In Vitro:
  Amsacrine blocks HERG currents in HEK 293 cells and Xenopus oocytes in a concentration-dependent manner, with IC50 values of 209.4 nm and 2.0 μM, respectively. Amsacrine causes a negative shift in the voltage dependence of both activation ( 7.6 mV) and inactivation ( 7.6 mV). HERG current block by amsacrine is not frequency dependent. In vitro studies of normal human lymphocytes with various concentrations of m-AMSA, show both increased levels of chromosomal aberrations, ranging from 8% to 100%, and increase SCEs, ranging from 1.5 times the normal at the lowest concentration studied (0.005 μg/mL) to 12 times the normal (0.25 μg/mL). Amsacrine-induced apoptosis of U937 cells is characterized by caspase-9 and caspase-3 activation, increased intracellular Ca2+ concentration, mitochondrial depolarization, and MCL1 down-regulation. Amsacrine induces MCL1 down-regulation by decreasing its stability. Further, amsacrine-treated U937 cells show AKT degradation and Ca2+-mediated ERK inactivation.

Storage & Handling

• Storage: store at low temperature | 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

CI880, CI-880, CI 880, AMSA, Amsacrine, Autophagy, acridinyl anisidide, Inhibitor, m-AMSA, inhibit, Potassium Channel, PotassiumChannel, Topo II, Topoisomerase

Compound Identifiers

PubChem CID

2179