|4-(9-吖啶基氨基)-N-(甲磺酰基)-间甲氧基苯胺|CsnPharm

CAS No.: 51264-14-3

Amsacrine/安吖啶 Catalog No. CSN18312

Synonyms: m-AMSA;acridinyl anisidide;AMSA

Amsacrine can intercalate into the DNA of tumor cells with antineoplastic activity.

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生物活性

描述Topoisomerase II is an essential enzyme that plays a role in virtually every cellular DNA process. This enzyme interconverts different topological forms of DNA by passing one nucleic acid segment through a transient double-stranded break generated in a second segment^[3].Amsacrine 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. 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^[4].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, Amsacrine (m-AMSA) has high incidences of clastogenicity and low incidences of aneugenicity during mitotic phases in vivo^[5]. In vitro studies of normal human lymphocytes with various concentrations of Amsacrine (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)^[6].Amsacrine (m-AMSA)-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 (m-AMSA) induces MCL1 down-regulation by decreasing its stability^[7].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00002658	Leukemia Neut... more >>ropenia Collapse <<	Phase 3	Unknown	-	United Kingdom ... more >> University of Wales College of Medicine Cardiff, Wales, United Kingdom, CF14 4XN Collapse <<
NCT00002719	Leukemia Neut... more >>ropenia Collapse <<	Phase 3	Completed	-	Italy ... more >> Azienda Policlinico Umberto Primo Rome, Italy, 00161 Collapse <<
NCT00840684	Leukemia	Phase 1 Phase 2	Completed	-	France ... more >> Marseille Institute of Cancer - Institut J. Paoli and I. Calmettes Marseille, France, 13273 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5416 mL
- 12.7078 mL
- 25.4156 mL
- 5 mM
- 0.5083 mL
- 2.5416 mL
- 5.0831 mL
- 10 mM
- 0.2542 mL
- 1.2708 mL
- 2.5416 mL

技术信息

CAS号

51264-14-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H19N3O3S

运输

蓝冰

分子量

393.46

别名

m-AMSA;acridinyl anisidide;AMSA;CI-880;SN-11841;Amsidine;Amsidyl;安吖啶

溶解度

DMSO	9.3 mg/mL (23.6 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00002658	Leukemia Neut... more >>ropenia Collapse <<	Phase 3	Unknown	-	United Kingdom ... more >> University of Wales College of Medicine Cardiff, Wales, United Kingdom, CF14 4XN Collapse <<
NCT00002719	Leukemia Neut... more >>ropenia Collapse <<	Phase 3	Completed	-	Italy ... more >> Azienda Policlinico Umberto Primo Rome, Italy, 00161 Collapse <<
NCT00840684	Leukemia	Phase 1 Phase 2	Completed	-	France ... more >> Marseille Institute of Cancer - Institut J. Paoli and I. Calmettes Marseille, France, 13273 Collapse <<
NCT00003436	Leukemia Myel... more >>odysplastic Syndromes Collapse <<	Phase 3	Completed	-	United Kingdom ... more >> Christie Hospital N.H.S. Trust Manchester, England, United Kingdom, M20 4BX Collapse <<
NCT02182596	Acute Myeloid Leukemia	Phase 1 Phase 2	Completed	-	France ... more >> Hopital Avicenne Bobigny, France CH Caen, France, 14033 Hopital Percy Clamart, France, 92141 CHU Creteil, France, 94010 CHU Lille, France, 59037 CH Limoges, France, 87042 Hopital Edouard Herriot Lyon, France CH Meaux, France, 77104 St Antoine Hospital Paris, France, 75012 Hopital Saint-Louis Paris, France CH Roubaix, France, 59100 CHU Rouen, France, 76038 CNLCC Saint-Cloud, France CH Versailles, France IGR Villejuif, France, 94805 Collapse <<
NCT01039363	Acute Myeloid Leukemia	Phase 2	Unknown	-	Korea, Republic of ... more >> Samsung Medical Center Not yet recruiting Seoul, Korea, Republic of, 135-710 Principal Investigator: Dong Hwan Won, M.D.,Ph.D. Collapse <<
NCT00180102	Leukemia, Nonlymphocytic, Acut... more >>e Collapse <<	Phase 4	Completed	-	Germany ... more >> Medical Department I, University Hospital Carl Gustav Carus Dresden, Germany, 01307 Collapse <<
NCT03765541	Relapsed or Refractory Acute M... more >>yeloid Leukemia Collapse <<	Phase 3	Not yet recruiting	January 2024	France ... more >> CHU de Grenoble Not yet recruiting Grenoble, France Contact: Jean-Yves CAHN, PhD CHU de Limoges Not yet recruiting Limoges, France Contact: Pascal TURLURE, MD Institut Paoli Calmettes Not yet recruiting Marseille, France Contact: Norbert VEY, PhD CHU de Montpellier Not yet recruiting Montpellier, France Contact: Hicheri Yosr, MD CHU de Nantes Not yet recruiting Nantes, France Contact: Pierre PETERLIN, MD CHU de Nîmes Not yet recruiting Nîmes, France Contact: Eric JOURDAN, MD CHU de Bordeaux Not yet recruiting Pessac, France Contact: Arnaud PIGNEUX, PhD CHU de Poitiers Not yet recruiting Poitiers, France Contact: Maria-Pilar GALLEGO-HERMANZ, MD Collapse <<
NCT01228331	Leukemia	Phase 2 Phase 3	Recruiting	September 2021	Germany ... more >> Krankenanstalten Gilead gCmbH Neurochirurgische Klinik Recruiting Bielefeld, Germany, 33617 Contact: Contact Person 49-521-144-2728 Klinikum Bremen-Mitte Recruiting Bremen, Germany, D-28205 Contact: Contact Person 49-421-497-5413 Universitaetsklinikum Duesseldorf Recruiting Duesseldorf, Germany, D-40225 Contact: Contact Person 49-211-81-17662 Klinik und Poliklinik Fuer Kinder-und Jugendmedizin - Universitaetsklinikum Greifswald Recruiting Greifswald, Germany, 17487 Contact: Contact Person 49-3834-86-6321 University Medical Center Hamburg - Eppendorf Recruiting Hamburg, Germany, D-20246 Contact: Contact Person 49-407-4105-2580 horstmann@uke.uni-hamburg.de Clinic for Bone Marrow Transplantation and Hematology and Oncology Recruiting Idar-Oberstein, Germany, D-55743 Contact: Contact Person 49-6781-66-1582 Klinikum Krefeld GmbH Recruiting Krefeld, Germany, D-47805 Contact: Contact Person 49-2151-322-375 Universitaets - Kinderklinik Recruiting Leipzig, Germany, D-04317 Contact: Contact Person 49-341-9726-113 Johannes Gutenberg University Recruiting Mainz, Germany, D-55101 Contact: Contact Person 49-6131-17-2642 Dr. von Haunersches Kinderspital der Universitaet Muenchen Recruiting Munich, Germany, D-80337 Contact: Contact Person 49-89-5160-2843 Staedtisches Krankenhaus Muenchen - Harlaching Recruiting Munich, Germany, D-81545 Contact: Contact Person 49-89-6210-2720 Klinik St. Hedwig-Kinderklinik Recruiting Regensburg, Germany, 93049 Contact: Contact Person 49-941-2080-493 Dr. Horst-Schmidt-Kliniken Recruiting Wiesbaden, Germany, D-65199 Contact: Contact Person 49-611-43-2564 Helios Kliniken Wuppertal University Hospital Recruiting Wuppertal, Germany, D-42283 Contact: Contact Person 49-202-896-2444 Collapse <<
NCT01324063	Leukemia	Phase 3	Completed	-	-
NCT01423175	Acute Myeloid Leukemia ... more >> MDS Collapse <<	Phase 2	Unknown	-	Germany ... more >> Hannover Medical School Recruiting Hannover, Germany, 30625 Contact: Arnold Ganser, Prof. Dr. ++49-511-532-3020 ganser.arnold@mh-hannover.de Universitaetsklinikum des Saarlandes Not yet recruiting Homburg/Saar, Germany, 66421 Contact: Michael Pfreundschuh, Prof. Dr. ++49-6841-16-23002 pfreundschuh@unikliniksaarland.de Universitaetsklinikum Leipzig AoeR Not yet recruiting Leipzig, Germany, 04103 Contact: Dietger Niederwieser, Prof. Dr. ++49-341-0713050 dietger.niederwieser@medizin.uni-leipzig.de Collapse <<

Amsacrine/安吖啶 Catalog No. CSN18312

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