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Amsacrine

Catalog No. T1206   CAS 51264-14-3
Synonyms: AMSA, m-AMSA, CI-880, acridinyl anisidide

Amsacrine (AMSA) (mAMSA) an antineoplastic agent which can intercalate into the DNA of tumor cells. Amsacrine also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II.

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Amsacrine Chemical Structure
Amsacrine, CAS 51264-14-3
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10 mg In stock $ 39.00
25 mg In stock $ 58.00
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1 mL * 10 mM (in DMSO) In stock $ 30.00
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Purity: 98.59%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Amsacrine (AMSA) (mAMSA) an antineoplastic agent which can intercalate into the DNA of tumor cells. Amsacrine also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II.
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[1]. 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)[3]. 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[4].
In vivo In animals treated with different doses of amsacrine (0.5-12 mg/kg), the frequencies of micronucleated polychromatic erythrocytes increase significantly after treatment with 9 and 12 mg/kg. Furthermore, the present study demonstrates for the first time that amsacrine has high incidences of clastogenicity and low incidences of aneugenicity whereas nocodazole has high incidences of aneugenicity and low incidences of clastogenicity during mitotic phases in vivo[2].
Synonyms AMSA, m-AMSA, CI-880, acridinyl anisidide
Molecular Weight 393.46
Formula C21H19N3O3S
CAS No. 51264-14-3

Storage

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

Solubility Information

DMSO: 50 mg/mL (127.08 mM)

TargetMolReferences and Literature

1. Thomas D, et al. Inhibition of cardiac HERG currents by the DNA topoisomerase II inhibitor amsacrine: mode of action. Br J Pharmacol. 2004 Jun;142(3):485-94. 2. Attia SM. Molecular cytogenetic evaluation of the mechanism of genotoxic potential of amsacrine and nocodazole in mouse bone marrow cells. J Appl Toxicol. 2013 Jun;33(6):426-33. 3. Kao-Shan CS, et al. Cytogenetic effects of amsacrine on human lymphocytes in vivo and in vitro. Cancer Treat Rep. 1984 Jul-Aug;68(7-8):1989-97. 4. Lee YC, et al. Amsacrine-induced apoptosis of human leukemia U937 cells is mediated by the inhibition of AKT- and ERK-induced stabilization of MCL1. Apoptosis. 2016 Oct 19. 5. Fu, Wan, et al. A novel acridine derivative,. LS-1-10 inhibits autophagic degradation and triggers apoptosis in colon cancer cells [J]. Cell death & disease. 2017 Oct 5;8(10):e3086.

TargetMolCitations

1. Fu W, Li X, Lu X, et al. A novel acridine derivative, LS-1-10 inhibits autophagic degradation and triggers apoptosis in colon cancer cells. Cell Death & Disease. 2017, 8(10): e3086-e3086

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Pediatric Drug Library Bioactive Compound Library Human Metabolite Library Autophagy Compound Library

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Keywords

Amsacrine 51264-14-3 Autophagy DNA Damage/DNA Repair Membrane transporter/Ion channel Potassium Channel Topoisomerase AMSA m-AMSA Inhibitor CI880 CI-880 acridinyl anisidide inhibit CI 880 inhibitor

 

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