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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。
Topoisomerase I inhibitor 5 Chemical Structure
CAS No. : 2513461-95-3
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 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].
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IC50 & Target |
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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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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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].
Shanghai Jinpan Biotech Co Ltd 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Zhong H, Zhao M, Wu C, Zhang J, Chen L, Sun J. Development of oxoisoaporphine derivatives with topoisomerase I inhibition and reversal of multidrug resistance in breast cancer MCF-7/ADR cells. Eur J Med Chem. 2022;235:114300.
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