上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
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 |
|
是否有货 |
|
| 100 mg |
|
询价 |
|
| 250 mg |
|
询价 |
|
| 500 mg |
|
询价 |
|
* 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].
|
IC50 & Target |
|
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].
上海金畔生物科技有限公司 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. |
|
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].
上海金畔生物科技有限公司 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 |
|
| Formula |
|
| 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.
|
| 参考文献 |
-
[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.
|
所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务
