80277-11-8
Chemical Structure
Amsacrine lactate
Synonym(s): m-AMSA lactate; Acridinyl anisidide lactate
- CAS No.: 80277-11-8
- Formula:C24H25N3O6S
- Molecular Weight:483.54
InChIKey: NYGZSXVEKMITFN-UHFFFAOYSA-N
SMILES: O=C(C(C)O)O.O=S(NC1=CC=C(C(OC)=C1)NC2=C3C=CC=CC3=NC4=C2C=CC=C4)(C)=O
Biological Activity: Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies[1][2][3][4].
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Amsacrine lactate | Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca2+-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies. | |||||||||||||||||||||
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- [1]. 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 : an international journal on programmed cell death. 2017 Mar;22(3):406-420. [Content Brief]
- [2]. Thomas D, et al. Inhibition of cardiac HERG currents by the DNA topoisomerase II inhibitor amsacrine: mode of action. British journal of pharmacology. 2004 Jun;142(3):485-94. [Content Brief]
- [3]. Attia SM. Molecular cytogenetic evaluation of the mechanism of genotoxic potential of amsacrine and nocodazole in mouse bone marrow cells. Journal of applied toxicology : JAT. 2013 Jun;33(6):426-33. [Content Brief]
- [4]. Kao-Shan CS, et al. Cytogenetic effects of amsacrine on human lymphocytes in vivo and in vitro. Cancer treatment reports. 1984;68(7-8):989-97. [Content Brief]
Keywords
