1. Cell Cycle/DNA Damage Autophagy
  2. Topoisomerase Autophagy
  3. Amsacrine

Amsacrine  (Synonyms: 安吖啶; m-AMSA; acridinyl anisidide)

目录号: HY-13551 纯度: 99.91%
COA 产品使用指南 技术支持

Amsacrine (m-AMSA; acridinyl anisidide) 是肿瘤细胞 DNA 嵌入剂,还能抑制拓扑异构酶 II。

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Amsacrine Chemical Structure

Amsacrine Chemical Structure

CAS No. : 51264-14-3

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Other Forms of Amsacrine:

查看 Topoisomerase 亚型特异性产品:

  • 生物活性

  • 实验参考方法

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  • 参考文献

生物活性

Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.

IC50 & Target[1]

Topoisomerase II

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
2008 IC50
4.31 μM
Compound: m-AMSA
Cytotoxicity against human 2008 cells after 72 hrs by MTT assay
Cytotoxicity against human 2008 cells after 72 hrs by MTT assay
[PMID: 19101158]
A2780 GI50
0.027 μM
Compound: m-AMSA
Growth inhibition of human A2780 cells incubated for 72 hrs by trypan blue assay
Growth inhibition of human A2780 cells incubated for 72 hrs by trypan blue assay
[PMID: 32435372]
A2780 IC50
0.1 μM
Compound: m-AMSA
Concentration required to inhibit the cell growth by 50 % after 96 hr A2780 leukemic cells.
Concentration required to inhibit the cell growth by 50 % after 96 hr A2780 leukemic cells.
[PMID: 7658436]
A-431 IC50
0.17 μM
Compound: 1, m-AMSA
Growth inhibition in human A431 cells after 72 hrs by trypan blue assay
Growth inhibition in human A431 cells after 72 hrs by trypan blue assay
[PMID: 21216603]
A-431 IC50
5.89 μM
Compound: m-AMSA
Cytotoxicity against human A431 cells after 72 hrs by MTT assay
Cytotoxicity against human A431 cells after 72 hrs by MTT assay
[PMID: 19101158]
A549 IC50
0.03 μM
Compound: 1
Inhibitory activity against A549 cell line using MTT assay(Wild type p53)
Inhibitory activity against A549 cell line using MTT assay(Wild type p53)
[PMID: 10780913]
A549 IC50
22.2 μM
Compound: m-Amsa
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33479643]
A549 IC50
3.52 μM
Compound: m-AMSA
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 19101158]
A549 IC50
5.96 μM
Compound: 2; m-AMSA
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 27060757]
CCRF-CEM IC50
0.03 μM
Compound: m-AMSA
Antiproliferative against human CCRF-CEM cells incubated for 72 hrs by MTT assay
Antiproliferative against human CCRF-CEM cells incubated for 72 hrs by MTT assay
[PMID: 31635931]
CCRF-CEM IC50
0.18 μM
Compound: 2; m-AMSA
Antiproliferative activity against human CCRF-CEM cells after 48 hrs by MTT assay
Antiproliferative activity against human CCRF-CEM cells after 48 hrs by MTT assay
[PMID: 27060757]
CCRF-CEM IC50
130 nM
Compound: amsacrine
Cytotoxicity against human CCRF-CEM cells after 72 hrs
Cytotoxicity against human CCRF-CEM cells after 72 hrs
[PMID: 18329887]
CHO-AA8 IC50
0.6 nM
Compound: Amsacrine
Inhibitory activity of compound for AA8 cells to reduce cell density by 50% (exposed to compound for 4 hours)
Inhibitory activity of compound for AA8 cells to reduce cell density by 50% (exposed to compound for 4 hours)
[PMID: 2909741]
COLO 205 IC50
1.1 μM
Compound: Amsacrine
Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay
Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay
[PMID: 22546208]
DLD-1 IC50
0.08 μM
Compound: amsacrine
Cytotoxicity against human DLD1 cells by Hoechst test
Cytotoxicity against human DLD1 cells by Hoechst test
[PMID: 18656367]
DLD-1 IC50
0.57 μM
Compound: amsacrine
Cytotoxicity against human DLD1 cells by resazurin reduction test
Cytotoxicity against human DLD1 cells by resazurin reduction test
[PMID: 18656367]
DU-145 IC50
0.3 μM
Compound: Amsacrine
Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay
Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay
[PMID: 22546208]
F460pv8/eto IC50
0.04 μM
Compound: 1
Inhibitory activity against F460pv8/eto cell line using MTT assay
Inhibitory activity against F460pv8/eto cell line using MTT assay
[PMID: 10780913]
Fibroblast IC50
2 μM
Compound: amsacrine
Cytotoxicity against human fibroblast cells by Hoechst test
Cytotoxicity against human fibroblast cells by Hoechst test
[PMID: 18656367]
Fibroblast IC50
4.2 μM
Compound: amsacrine
Cytotoxicity against human fibroblast cells by resazurin reduction test
Cytotoxicity against human fibroblast cells by resazurin reduction test
[PMID: 18656367]
HCC1937 IC50
7.85 μM
Compound: m-AMSA
Antiproliferative activity against human HCC1937 cells harboring BRCA1 mutant after 72 hrs by MTT assay
Antiproliferative activity against human HCC1937 cells harboring BRCA1 mutant after 72 hrs by MTT assay
[PMID: 28763648]
HCT-116 IC50
< 1 μM
Compound: m-AMSA
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
[PMID: 29954683]
HCT-116 IC50
0.7 μM
Compound: m-AMSA
Cytotoxicity against human HCT116 cells by XTT assay
Cytotoxicity against human HCT116 cells by XTT assay
[PMID: 17368022]
HCT-116 IC50
0.93 μM
Compound: 2; m-AMSA
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
[PMID: 27060757]
HCT-116 IC50
3.89 μM
Compound: m-AMSA
Antiproliferative activity against human HCT116 cells expressing topoisomerase-1 after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells expressing topoisomerase-1 after 72 hrs by MTT assay
[PMID: 28763648]
HCT-15 IC50
0.3 μM
Compound: Amsacrine
Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT15 cells after 72 hrs by MTT assay
[PMID: 22546208]
HCT-8 IC50
0.3 μM
Compound: Amsacrine
Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT8 cells after 72 hrs by MTT assay
[PMID: 22546208]
HEK293 IC50
5 μM
Compound: amsacrine
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
[PMID: 18788725]
HeLa IC50
0.012 μM
Compound: 1, m-AMSA
Growth inhibition in human HeLa cells after 72 hrs by trypan blue assay
Growth inhibition in human HeLa cells after 72 hrs by trypan blue assay
[PMID: 21216603]
HeLa IC50
0.012 μM
Compound: m-amsacrine
Antiproliferative activity against human HeLa cells after 72 hrs by trypan blue test
Antiproliferative activity against human HeLa cells after 72 hrs by trypan blue test
[PMID: 18077173]
HeLa GI50
0.031 μM
Compound: m-AMSA
Growth inhibition of human HeLa cells incubated for 72 hrs by trypan blue assay
Growth inhibition of human HeLa cells incubated for 72 hrs by trypan blue assay
[PMID: 32435372]
HeLa IC50
0.34 μM
Compound: 2; m-AMSA
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 27060757]
HeLa EC50
0.72 μM
Compound: m-AMSA
Tested for inhibitory activity against Topoisomerase II isolated from HeLa cells by using SDS-K+ precipitation method
Tested for inhibitory activity against Topoisomerase II isolated from HeLa cells by using SDS-K+ precipitation method
10.1016/S0960-894X(00)80048-7
HeLa EC50
0.72 μM
Compound: mAMSA
Compound was tested for topoisomerase II inhibition in purified HeLa cells by SDS/K+ precipitation method
Compound was tested for topoisomerase II inhibition in purified HeLa cells by SDS/K+ precipitation method
10.1016/0960-894X(95)00044-T
HeLa EC50
0.72 μM
Compound: m-AMSA
Inhibitory activity in a cell-free assay of DNA cleavage mediated by purified HeLa cell topoisomerase II.
Inhibitory activity in a cell-free assay of DNA cleavage mediated by purified HeLa cell topoisomerase II.
10.1016/0960-894X(95)00043-S
HeLa EC50
0.72 μM
Compound: 5 (m-AMSA)
Tested for inhibition of topoisomerase II isolated from HeLa cells by DNA-cleavage assay
Tested for inhibition of topoisomerase II isolated from HeLa cells by DNA-cleavage assay
[PMID: 8410993]
HeLa IC50
19.19 μM
Compound: m-AMSA
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay
[PMID: 28511910]
HeLa IC50
9.5 μM
Compound: m-AMSA
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
[PMID: 19364657]
HeLa IC50
9.5 μM
Compound: Amsacrine
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
[PMID: 18035542]
HepG2 IC50
5.21 μM
Compound: m-AMSA
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 28511910]
HL-60 IC50
0.0051 μM
Compound: m-amsacrine
Antiproliferative activity against human HL60 cells after 72 hrs by trypan blue test
Antiproliferative activity against human HL60 cells after 72 hrs by trypan blue test
[PMID: 18077173]
HL-60 IC50
0.006 μM
Compound: 1, m-AMSA
Growth inhibition in human HL60 cells after 72 hrs by trypan blue assay
Growth inhibition in human HL60 cells after 72 hrs by trypan blue assay
[PMID: 21216603]
HL-60 IC50
0.08 μM
Compound: Amsacrine
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
[PMID: 22546208]
HL-60 IC50
1.15 μM
Compound: m-AMSA
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 19101158]
HT-1080 GI50
1.6 μM
Compound: m-Amsa
Cytocidal activity against human HT1080 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytocidal activity against human HT1080 cells assessed as growth inhibition after 48 hrs by SRB assay
[PMID: 22503207]
HT-1080 GI50
1.6 μM
Compound: m-Amsa
Antiproliferative activity against human HT1080 cells after 48 hrs by SRB assay
Antiproliferative activity against human HT1080 cells after 48 hrs by SRB assay
[PMID: 18403058]
HT-29 GI50
16.8 μM
Compound: m-Amsa
Cytocidal activity against human HT-29 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytocidal activity against human HT-29 cells assessed as growth inhibition after 48 hrs by SRB assay
[PMID: 22503207]
HT-29 GI50
16.8 μM
Compound: m-Amsa
Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay
Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay
[PMID: 18403058]
HT-29 IC50
559 nM
Compound: m-AMSA
Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay
[PMID: 2778449]
Jurkat IC50
< 1 μM
Compound: 3
Concentration required to reduce growth of human jurkat leukemia cells to 50% of control cultures, determined using a 72 hr continuous exposure
Concentration required to reduce growth of human jurkat leukemia cells to 50% of control cultures, determined using a 72 hr continuous exposure
[PMID: 8182707]
Jurkat IC50
0.02 μM
Compound: amsacrine
Cytotoxicity against human Jurkat cells by Hoechst test
Cytotoxicity against human Jurkat cells by Hoechst test
[PMID: 18656367]
Jurkat IC50
0.08 μM
Compound: amsacrine
Cytotoxicity against human Jurkat cells by resazurin reduction test
Cytotoxicity against human Jurkat cells by resazurin reduction test
[PMID: 18656367]
K562 IC50
0.023 μM
Compound: amsacrine (m-AMSA)
Cytotoxicity against human K562 cells after 5 days by XTT assay
Cytotoxicity against human K562 cells after 5 days by XTT assay
[PMID: 18076140]
K562 IC50
0.71 μM
Compound: m-AMSA
Antiproliferative against human K562 cells incubated for 72 hrs by MTT assay
Antiproliferative against human K562 cells incubated for 72 hrs by MTT assay
[PMID: 31635931]
K562 IC50
0.88 μM
Compound: m-AMSA
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
[PMID: 28511910]
K562 IC50
13.8 μM
Compound: m-Amsa
Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33479643]
K562 IC50
19.9 μM
Compound: m-AMSA
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
[PMID: 19364657]
K562 IC50
19.9 μM
Compound: Amsacrine
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
[PMID: 18035542]
M21 GI50
49.6 μM
Compound: m-Amsa
Cytocidal activity against human M21 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytocidal activity against human M21 cells assessed as growth inhibition after 48 hrs by SRB assay
[PMID: 22503207]
M21 GI50
49.6 μM
Compound: m-Amsa
Antiproliferative activity against human M21 cells after 48 hrs by SRB assay
Antiproliferative activity against human M21 cells after 48 hrs by SRB assay
[PMID: 18403058]
M4Beu cell line IC50
0.4 μM
Compound: amsacrine
Cytotoxicity against human M4Beu cells by Hoechst test
Cytotoxicity against human M4Beu cells by Hoechst test
[PMID: 18656367]
M4Beu cell line IC50
0.74 μM
Compound: amsacrine
Cytotoxicity against human M4Beu cells by resazurin reduction test
Cytotoxicity against human M4Beu cells by resazurin reduction test
[PMID: 18656367]
MCF7 IC50
0.075 μM
Compound: 1
Inhibitory activity against MCF-7 wt cell line using MTT assay (ER+,pgR+,wildtype p53)
Inhibitory activity against MCF-7 wt cell line using MTT assay (ER+,pgR+,wildtype p53)
[PMID: 10780913]
MCF7 IC50
0.075 μM
Compound: 1
Inhibitory activity against MCF7wt cell line using MTT assay
Inhibitory activity against MCF7wt cell line using MTT assay
[PMID: 10780913]
MCF7 IC50
0.91 μM
Compound: m-Amsa
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31421632]
MCF7 IC50
21.7 μM
Compound: m-AMSA
Cytotoxicity against human MCF7 cells by XTT assay
Cytotoxicity against human MCF7 cells by XTT assay
[PMID: 18093835]
MCF7 IC50
21.7 μM
Compound: m-AMSA
Cytotoxicity against human MCF7 cells by XTT assay
Cytotoxicity against human MCF7 cells by XTT assay
[PMID: 17368022]
MCF7 IC50
26.76 μM
Compound: 2; m-AMSA
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 27060757]
MCF7 IC50
5.13 μM
Compound: m-AMSA
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 19101158]
MCF7 GI50
5.6 μM
Compound: m-Amsa
Cytocidal activity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytocidal activity against human MCF7 cells assessed as growth inhibition after 48 hrs by SRB assay
[PMID: 22503207]
MCF7 GI50
5.6 μM
Compound: m-Amsa
Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay
Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay
[PMID: 18403058]
MCF7 IC50
8.7 μM
Compound: m-AMSA
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 28763648]
MDA-MB-231 IC50
0.14 μM
Compound: 1
Inhibitory activity against MDA-231 cell line using MTT assay (ER-,EGFR+,mutant p53)
Inhibitory activity against MDA-231 cell line using MTT assay (ER-,EGFR+,mutant p53)
[PMID: 10780913]
MDA-MB-231 IC50
10.05 μM
Compound: m-AMSA
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 29954683]
MDA-MB-468 IC50
0.49 μM
Compound: 1
Inhibitory activity against MDA-468 cell line using MTT assay (ER-, amplified EGFR, mutant p53)
Inhibitory activity against MDA-468 cell line using MTT assay (ER-, amplified EGFR, mutant p53)
[PMID: 10780913]
MDA-MB-468 IC50
8.5 μM
Compound: m-AMSA
Cytotoxicity against human MDA-MB468 cells by XTT assay
Cytotoxicity against human MDA-MB468 cells by XTT assay
[PMID: 17368022]
MRC5 IC50
15.4 μM
Compound: m-Amsa
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33479643]
MSTO-211H GI50
0.019 μM
Compound: m-AMSA
Growth inhibition of human MSTO-211H cells incubated for 72 hrs by trypan blue assay
Growth inhibition of human MSTO-211H cells incubated for 72 hrs by trypan blue assay
[PMID: 32435372]
NCI/ADR-RES IC50
1.165 μM
Compound: 1
Inhibitory activity against MCF-7/adr cell line using MTT assay
Inhibitory activity against MCF-7/adr cell line using MTT assay
[PMID: 10780913]
NCI-H226 IC50
1.01 μM
Compound: 1
Inhibitory activity against NCI-H226 cell line using MTT assay(mutant p53)
Inhibitory activity against NCI-H226 cell line using MTT assay(mutant p53)
[PMID: 10780913]
NCI-H322M IC50
0.21 μM
Compound: 1
Inhibitory activity against NCI-H322 cell line using MTT assay(mutant p53)
Inhibitory activity against NCI-H322 cell line using MTT assay(mutant p53)
[PMID: 10780913]
NCI-H358 IC50
0.15 μM
Compound: 1
Inhibitory activity against NCI-H358 cell line using MTT assay(mutant p53)
Inhibitory activity against NCI-H358 cell line using MTT assay(mutant p53)
[PMID: 10780913]
NCI-H460 IC50
0.06 μM
Compound: 1
Inhibitory activity against NCI-H460 cell line using MTT assay
Inhibitory activity against NCI-H460 cell line using MTT assay
[PMID: 10780913]
NCI-H460 IC50
0.06 μM
Compound: 1
Inhibitory activity against NCI-H460 cell line using MTT assay(Wild type p53)
Inhibitory activity against NCI-H460 cell line using MTT assay(Wild type p53)
[PMID: 10780913]
NCI-H460 IC50
0.2 μM
Compound: 1
Inhibitory activity against H460pv8 cell line using MTT assay
Inhibitory activity against H460pv8 cell line using MTT assay
[PMID: 10780913]
NCI-H647 IC50
0.07 μM
Compound: 1
Inhibitory activity against NCI-H647 cell line using MTT assay(mutant p53)
Inhibitory activity against NCI-H647 cell line using MTT assay(mutant p53)
[PMID: 10780913]
OVCAR-8 IC50
1.4 μM
Compound: Amsacrine
Antiproliferative activity against human OVCAR8 cells after 72 hrs by MTT assay
Antiproliferative activity against human OVCAR8 cells after 72 hrs by MTT assay
[PMID: 22546208]
P388 IC50
0.15 μM
Compound: mAMSA
In Vitro Cytotoxicity was measured by quantifying clonogenic survival in soft agar following a 1 hr transient exposure of P388 mouse leukemia cells to compound
In Vitro Cytotoxicity was measured by quantifying clonogenic survival in soft agar following a 1 hr transient exposure of P388 mouse leukemia cells to compound
10.1016/0960-894X(96)00230-2
P388 IC50
0.15 μM
Compound: mAMSA
In vitro cytotoxicity measured by quantifying clonogenic survival in soft agar following a 1-hour transient exposure of p388 mouse leukemia cells.
In vitro cytotoxicity measured by quantifying clonogenic survival in soft agar following a 1-hour transient exposure of p388 mouse leukemia cells.
[PMID: 9733489]
P388 IC50
229 nM
Compound: m-AMSA
Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay
Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay
[PMID: 2778449]
PBMC IC50
21.7 μM
Compound: Amsacrine
Cytotoxicity against human PBMC after 72 hrs by alamar blue assay
Cytotoxicity against human PBMC after 72 hrs by alamar blue assay
[PMID: 22546208]
PC-3 IC50
3.3 μM
Compound: Amsacrine
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
[PMID: 22546208]
RAW264.7 CC50
95.5 μM
Compound: m-Amsa
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31421632]
SF-295 IC50
0.5 μM
Compound: Amsacrine
Antiproliferative activity against human SF295 cells after 72 hrs by MTT assay
Antiproliferative activity against human SF295 cells after 72 hrs by MTT assay
[PMID: 22546208]
SK-BR-3 IC50
0.06 μM
Compound: 1
Inhibitory activity against SKBR-3 cell line using MTT assay (ER-amplified erB2,mutant p53)
Inhibitory activity against SKBR-3 cell line using MTT assay (ER-amplified erB2,mutant p53)
[PMID: 10780913]
SW480 IC50
27.7 μM
Compound: m-AMSA
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
[PMID: 19364657]
SW480 IC50
27.7 μM
Compound: Amsacrine
Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay
Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay
[PMID: 18035542]
SW-620 IC50
0.3 μM
Compound: Amsacrine
Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay
Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay
[PMID: 22546208]
SW-620 IC50
16.7 μM
Compound: m-AMSA
Cytotoxicity against human SW620 cells after 72 hrs by MTT assay
Cytotoxicity against human SW620 cells after 72 hrs by MTT assay
[PMID: 19364657]
SW-620 IC50
16.7 μM
Compound: Amsacrine
Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay
Antiproliferative activity against human SW620 cells after 72 hrs by MTT assay
[PMID: 18035542]
T47D IC50
0.22 μM
Compound: 1
Inhibitory activity against T47D cell line using MTT assay (ER+,mutant p53)
Inhibitory activity against T47D cell line using MTT assay (ER+,mutant p53)
[PMID: 10780913]
T47D IC50
0.94 μM
Compound: m-Amsa
Cytotoxicity against human T47D cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human T47D cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31421632]
U-937 IC50
0.08 μM
Compound: m-AMSA
Antiproliferative against human U937 cells incubated for 72 hrs by MTT assay
Antiproliferative against human U937 cells incubated for 72 hrs by MTT assay
[PMID: 31635931]
U-937 IC50
0.61 μM
Compound: m-AMSA
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
[PMID: 29954683]
U-937 IC50
0.61 μM
Compound: m-AMSA
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
Antiproliferative activity against human U937 cells after 48 hrs by MTT assay
[PMID: 28511910]
V79 IC50
5.8 μM
Compound: Amsacrine
Cytotoxicity against chinese hamster V79 cells after 72 hrs by MTT assay
Cytotoxicity against chinese hamster V79 cells after 72 hrs by MTT assay
[PMID: 22546208]
ZR-75-1 IC50
0.18 μM
Compound: 1
Inhibitory activity against ZR-75-1 cell line using MTT assay (ER+,pgr+,mutant p53)
Inhibitory activity against ZR-75-1 cell line using MTT assay (ER+,pgr+,mutant p53)
[PMID: 10780913]
体外研究
(In Vitro)

Amsacrine (m-AMSA) 以浓度依赖性方式阻断 HEK 293 细胞和爪蟾卵母细胞中的 HERG 电流,IC50 值分别为 209.4 nm 和 2.0 μM。Amsacrine 会导致激活 (-7.6 mV) 和失活 (-7.6 mV) 的电压依赖性发生负偏移。Amsacrine对 HERG 电流的阻断与频率无关[1]。使用不同浓度的 Amsacrine 对正常人淋巴细胞进行的体外研究表明,染色体畸变水平增加,范围从 8% 到 100%,并且 SCEs 增加,在研究的最低浓度下是正常水平的 1.5 倍 (0.005 μg/mL) 至正常值 (0.25 μg/mL) 的 12 倍[3]。Amsacrine 诱导的 U937 细胞凋亡的特征在于 caspase-9 和 caspase-3 激活、细胞内 Ca2+ 浓度增加、线粒体去极化和 MCL1 下调。Amsacrine 通过降低其稳定性来诱导 MCL1 下调。此外,Amsacrine 处理的 U937 细胞显示出 AKT 降解和 Ca2+ 介导的 ERK 失活[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

在用不同剂量的 Amsacrine (0.5-12 mg/kg) 处理的动物中,微核多染红细胞的频率在用 9 和 12 mg/kg 处理后显著增加。此外,本研究首次证明 Amsacrine (m-AMSA) 在体内有丝分裂期具有高致染色体断裂发生率和低致染色体断裂发生率,而诺考达唑在有丝分裂期具有高致染色体断裂发生率和低致染色体断裂发生率[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

393.46

Formula

C21H19N3O3S

CAS 号
性状

固体

颜色

Orange to red

中文名称

安吖啶;胺苯吖啶

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 9.3 mg/mL (23.64 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5416 mL 12.7078 mL 25.4155 mL
5 mM 0.5083 mL 2.5416 mL 5.0831 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.35 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.95%

参考文献
Animal Administration
[2]

Amsacrine (m-AMSA) is investigated in three separated experiments. In the first experiment, animals are treated by intraperitoneal injection with 0.5, 1.5 and 4.5 mg/kg of amsacrine and bone marrow is sampled 24 h after treatment. Preliminary negative MN results at this sampling time lead to the use of 30 h sampling time for amsacrine. Thus, in the second experiment, mice are treated with 0.5, 1.5 and 4.5 mg/kg of Amsacrine (m-AMSA) and bone marrow is sampled 30 h after treatment. The doses and sampling times for amsacrine are chosen by reference to earlier studies and the selected doses are within the dose range used for human chemotherapy. The results again show that the micronuclei frequency in the bone marrow of mice is not affected by treatment with any of the selected doses of the test agent, at 30 h sampling time, thus, in the third experiment, mice are treated with 6, 9 and 12 mg/kg of amsacrine and bone marrow is sampled 24 and 30 h after treatment.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5416 mL 12.7078 mL 25.4155 mL 63.5389 mL
5 mM 0.5083 mL 2.5416 mL 5.0831 mL 12.7078 mL
10 mM 0.2542 mL 1.2708 mL 2.5416 mL 6.3539 mL
15 mM 0.1694 mL 0.8472 mL 1.6944 mL 4.2359 mL
20 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1769 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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