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

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.

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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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Topoisomerase I/II inhibitor 4 Related Antibodies

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Description

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].

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].

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

Topoisomerase I/II inhibitor 4 Related Antibodies

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.
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].

MedChemExpress (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
Molecular Weight

511.49

Formula

C27H21N5O6
CAS No.
SMILES

O=C1C2=C(C(C3=C1C4=C(C=CC=C4)N3CC5=CN([C@H]6O[C@@H]([C@H](C6)O)CO)N=N5)=O)C7=C([N+]([O-])=C2)C=CC=C7
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Topoisomerase I/II inhibitor 4 Related Classifications

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    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/II inhibitor 43031403-77-4TopoisomeraseApoptosistopoisomerase Itopoisomerase IIapoptosisanticancerInhibitorinhibitorinhibit

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