1. Cell Cycle/DNA Damage Apoptosis
  2. Topoisomerase Apoptosis
  3. Topoisomerase I/II inhibitor 4

Topoisomerase I/II inhibitor 4 

目录号: HY-149002
产品使用指南

Topoisomerase I/II inhibitor 4 (compound F16) 是一种有效的拓扑异构酶 I (Topo I) 和 II (Topo II) 双抑制剂。Topoisomerase I/II inhibitor 4 可以抑制细胞增殖、侵袭和迁移,诱导细胞凋亡 (apoptosis)。Topoisomerase I/II inhibitor 4 可用于肝癌的研究。

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Topoisomerase I/II inhibitor 4 Chemical Structure

Topoisomerase I/II inhibitor 4 Chemical Structure

CAS No. : 3031403-77-4

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查看 Topoisomerase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research[1].

体外研究
(In Vitro)

Topoisomerase I/II inhibitor 4 (compound F16) (0-100 μM) could intercalate into DNA to inhibit enzymatic activity and inhibit Topo I and II activities in a dose-dependent manner[1].
Topoisomerase I/II inhibitor 4 (compound F16) shows a high-expression level of Topo I and II enzymes in A375 and HCT116 cells and exhibits potent anti-proliferative activity with IC50 values of 20 and 50 nM, respectively, 10-fold lower than L02[1].
Topoisomerase I/II inhibitor 4 (compound F16) (0-40 nM, A375 cell) inhibits cancer cell colony formation, invasion, migration and induces cell apoptosis[1].

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

Cell Cycle Analysis[1]

Cell Line: A375 cells
Concentration: 20, 40 and 80 nM
Incubation Time: 24 hours
Result: The cell cycle blocked at the S phase in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: A375 cells
Concentration: 40, 80 and 120 nM
Incubation Time: 8, 16 and 24 hours
Result: Induced apoptosis rates for 8, 16 and 24 h were 7.14, 23.78 and 36.21%, respectively. Induced apoptosis rates for 40, 80 and 120 nM were 23.26, 36.21 and 55.94%, respectively.

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 40, 80 and 120 nM
Incubation Time: 24 hours
Result: The expression levels of Ccaspase-3, C-caspase-8, C-caspase-9, Bad and Bax increased in a dose-dependent manner, the Bcl-2 expression was obviously decreased.
体内研究
(In Vivo)

Topoisomerase I/II inhibitor 4 (compound F16) (10-50 mg/kg; i.v.; per 2 days, for 7 days) suppresses tumor growth in the A375 Xenograft Model[1].
Topoisomerase I/II inhibitor 4 (compound F16) of the plasma clearance rate (CL) was 7-fold lower than that of VP-16(0.007 L/min/kg). Topoisomerase I/II inhibitor 4 has a delayed elimination half-life of 151 min[1].

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

Animal Model: Female BALB/c nude mice (5−6 weeks)[1]
Dosage: 10 and 20 mg/kg
Administration: Intravenous injection; Per 2 days, for 14 days.
Result: Inhibited tumor growth in a melanoma xenograft mouse model and no apparent loss in body weight.
Animal Model: Kunming male mice [1]
Dosage: 10 mg/kg
Administration: Intravenous injection; for 5 , 15 , 30 , 60 , 120 , 240 and 360 min.
Result: 1.19
Parameter F16 VP-16
Dose (i.v.) mg/kg 10 10
Cmax (ng/mL) 26952 17712
Tmax (min) 5 5
AUCplasma (min*ng/mL) 2878363 409528
T1/2 (min) 151 45
Vd (L/Kg) 0.2341 0.432
CL (L/min/kg) 0.001 0.007
分子量

511.49

Formula

C27H21N5O6

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

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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.

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Topoisomerase I/II inhibitor 4
目录号:
HY-149002
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