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Cat. No.: HY-149002

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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.

For research use only. We do not sell to patients.

CAS No.: 3031403-77-4
Formula: C₂₇H₂₁N₅O₆
Molecular Weight:511.49

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

Topoisomerase I/II inhibitor 4 Chemical Structure

CAS No.: 3031403-77-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All Topoisomerase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.02 μM Compound: F16	Cytotoxicity against human A-375 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay Cytotoxicity against human A-375 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay	[PMID: 35612499]
A549	IC₅₀	0.12 μM Compound: F16	Cytotoxicity against human A549 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay	[PMID: 35612499]
HCT-116	IC₅₀	0.05 μM Compound: F16	Antiproliferative activity against doxorubicin sensitive human HCT-116 cells measured after 72 hrs by MTT assay Antiproliferative activity against doxorubicin sensitive human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 35612499]
HCT-116	IC₅₀	0.05 μM Compound: F16	Cytotoxicity against human HCT-116 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay	[PMID: 35612499]
HCT-116	IC₅₀	0.07 μM Compound: F16	Antiproliferative activity against doxorubicin resistant human HCT-116 cells measured after 72 hrs by MTT assay Antiproliferative activity against doxorubicin resistant human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 35612499]
HEK-293T	IC₅₀	0.82 μM Compound: F16	Cytotoxicity against human HEK293T cells measured after 72 hrs by MTT assay Cytotoxicity against human HEK293T cells measured after 72 hrs by MTT assay	[PMID: 35612499]
L02	IC₅₀	0.63 μM Compound: F16	Cytotoxicity against human L02 cells measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells measured after 72 hrs by MTT assay	[PMID: 35612499]
MCF7	IC₅₀	0.11 μM Compound: F16	Cytotoxicity against human MCF7 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay	[PMID: 35612499]
MDA-MB-231	IC₅₀	0.13 μM Compound: F16	Cytotoxicity against human MDA-MB-231 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells expressing high level of topoisomerase I/II measured after 72 hrs by MTT assay	[PMID: 35612499]
SH-SY5Y	IC₅₀	0.15 μM Compound: F16	Cytotoxicity against human SH-SY5Y cells expressing low level of topoisomerase I/II measured after 72 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells expressing low level of topoisomerase I/II measured after 72 hrs by MTT assay	[PMID: 35612499]

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.

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
C_max (ng/mL)	26952	17712
T_max (min)	5	5
AUC_plasma (min*ng/mL)	2878363	409528
T_1/2 (min)	151	45
Vd (L/Kg)	0.2341	0.432
CL (L/min/kg)	0.001	0.007

Chemical Information

CAS No. 3031403-77-4
Molecular Weight 511.49
Formula C₂₇H₂₁N₅O₆
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yang X, et al. Optimization of the Natural Product Calothrixin A to Discover Novel Dual Topoisomerase I and II Inhibitors with Improved Anticancer Activity. J Med Chem. 2022 Jun 9;65(11):8040-8061. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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