2. Cell Cycle/DNA Damage Apoptosis
  3. Topoisomerase DNA/RNA Synthesis Apoptosis
  4. Topoisomerase I inhibitor 5

Topoisomerase I inhibitor 5 是一种有效的拓扑异构酶 (topoisomerase) 抑制剂。Topoisomerase I inhibitor 5 能干扰 DNA，显著抑制 Topoisomerase I 活性。Topoisomerase I inhibitor 5 能将细胞周期阻滞在 G1 期，诱导 MCF-7 细胞凋亡 (apoptosis)。Topoisomerase I inhibitor 5 具有逆转 P-gp 介导的阿霉素耐药性的效力。

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Topoisomerase I inhibitor 5 Chemical Structure

Topoisomerase I inhibitor 5 Chemical Structure

CAS No. : 2513461-95-3

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Topoisomerase I inhibitor 5 相关抗体

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin[1].

IC50 & Target

Topoisomerase I[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
2.39 μM
Compound: 14
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: 35339100]
HepG2 IC50
4.88 μM
Compound: 14
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: 35339100]
L02 IC50
36.52 μM
Compound: 14
Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
[PMID: 35339100]
MCF7 IC50
1.32 μM
Compound: 14
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: 35339100]
MDA-MB-231 IC50
2.42 μM
Compound: 14
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: 35339100]
NCI/ADR-RES IC50
0.9 μM
Compound: 14
Reversal of multidrug resistant activity in human MCF7/ADR cells after 48 hrs by MTT assay
Reversal of multidrug resistant activity in human MCF7/ADR cells after 48 hrs by MTT assay
[PMID: 35339100]
NCI/ADR-RES IC50
7.64 μM
Compound: 14
Antiproliferative activity against human MCF7/ADR cells after 48 hrs by MTT assay
Antiproliferative activity against human MCF7/ADR cells after 48 hrs by MTT assay
[PMID: 35339100]
体外研究
(In Vitro)

Topoisomerase I inhibitor 5 (compound 14) (0-50 μM; 48 hours) exhibits antiproliferation activity against cancer cell lines and lower cytotoxicity in normal cells[1].
Topoisomerase I inhibitor 5 (2-8 μM; 24 hours) induces MCF-7 cell cycle arrest at the G1 phase[1].
Topoisomerase I inhibitor 5 (2-8 μM; 48 hours) increases the apoptotic rate of MCF-7/ADR and MCF-7 cells[1].
Topoisomerase I inhibitor 5 (1.5-6 μM; 24 hours) increases the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulates the level of anti-apoptotic protein, up-regulates the levels of pro-apoptotic proteins in MCF-7/ADR[1].
Topoisomerase I inhibitor 5 (0.1 μM; 24 hours) induces cell apoptosis by promoting the accumulation of ROS in MCF-7/ADR cell[1].
Topoisomerase I inhibitor 5 (10 μg/ml; 24 hours) increases the accumulation of the ADR and Rh123 in MCF-7/ADR cells[1].
Topoisomerase I inhibitor 5 (5, 10 and 20 μM; 24 hours) reduces the expression degree of P-gp by 14.95% and 18.10% in MCF-7/ADR cells at 10 and 20 μM[1].

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

Topoisomerase I inhibitor 5 相关抗体:

Cell Proliferation Assay

Cell Line: A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR and LO2 cells[1]
Concentration: 0-50 μM
Incubation Time: 48 hours
Result: Exhibited antiproliferation activity against cancer cell lines, with IC50s of 2.39 ± 0.23 μM, 4.88 ± 0.29 μM, 1.32 ± 0.14 μM, 7.64 ± 0.35 μM and 2.42 ± 0.14 μM in A549, HepG-2, MCF-7, MDA-MB-231, MCF-7/ADR, respectively; and has lower cytotoxicity in LO2 cells with IC50 of 36.52 ± 2.36 μM.

Cell Cycle Analysis

Cell Line: MCF-7[1]
Concentration: 2, 4 and 8 μM
Incubation Time: 24 hours
Result: Induced MCF-7 cell cycle arrest at the G1 phase.

Apoptosis Analysis

Cell Line: MCF-7 and MCF-7/ADR cells[1]
Concentration: 2, 4 and 8 μM
Incubation Time: 48 hours
Result: Induced apoptosis in a dose-dependent manner in MCF-7 cells, and increased the apoptotic rate of the cells from 2.8% to 15.2% in MCF-7/ADR.

Western Blot Analysis

Cell Line: MCF-7[1]
Concentration: 1.5, 3 and 6 μM in MCF-7; 5, 10, and 20 μM in MCF-7/ADR
Incubation Time: 24 hours
Result: Increased the expression degree of cleaved-caspase-3 and cleaved-PARP in MCF-7; down-regulated the level of anti-apoptotic protein bcl-2, up-regulated the levels of pro-apoptotic proteins bax and bad in MCF-7/ADR.
体内研究
(In Vivo)

Topoisomerase I inhibitor 5 (1 mg/kg and 10 mg/kg; IV; every two days, for 21 days) decreases the tumor growth significantly[1].

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

Animal Model: Bal b/c nude mice (injected with 106 MCF-7 cells in the left flank for 7 days)[1]
Dosage: 1 mg/kg and 10 mg/kg
Administration: IV; every two days, for 21 days
Result: Decreased the tumor growth significantly and the tumor inhibition ratio reached to 32.4% at 1 mg/kg and 7.2% at 10 mg/kg.
分子量

372.46

Formula

C24H24N2O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Topoisomerase I inhibitor 5 相关分类

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  • 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.

Keywords:

Topoisomerase I inhibitor 52513461-95-3Topoisomerase I inhibitor5Topoisomerase I inhibitor-5TopoisomeraseDNA/RNA SynthesisApoptosisOxoisoaporphine derivativesBreast cancerAntitumorP-gpMCF-7/ADR cellsInhibitorinhibitorinhibit

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