2. Cell Cycle/DNA Damage NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. Topoisomerase Reactive Oxygen Species Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis
  4. Topoisomerase I inhibitor 17

Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice.

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Topoisomerase I inhibitor 17 Chemical Structure

Topoisomerase I inhibitor 17 Chemical Structure

CAS No. : 2413582-45-1

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Topoisomerase I inhibitor 17 Related Antibodies

Top Publications Citing Use of Products

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Topoisomerase Topo I Topo II

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

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cIAP cIAP-1 cIAP-2 XIAP

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Description

Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice[1].

IC50 & Target[1]

Bax

 

Bcl-2

 

Top1

 

XIAP

 

In Vitro

Topoisomerase I inhibitor 17 (5-500 nM, 72 h) is antiproliferative to four cancer cells (HepG2, A549, HeLa and HCT116) with IC50s of 136.6, 33.7, 72.9 and 36.1 nM, respectively[1].
Topoisomerase I inhibitor 17 is translocated across the Caco-2 cell monolayer with an apparent permeability coefficient of 2.24 μcm/s from apical to basolateral (0.5-1.0 μM, 4 h), with viability of Caco-2 cells greater than 90% (0.2-1.0 μM, 4 h)[1].
Topoisomerase I inhibitor 17 (5-100 nM, 12-72 h) significantly inhibits proliferation-induced colony formation, concentration-dependently inhibits HCT116 cell migration, and increases ROS generation[1].
Topoisomerase I inhibitor 17 (0-50 μM, 48 h) induces apoptosis and cell cycle arrest in a dose-dependent manner and blocks the progression of the G2/M checkpoint in HCT116 cells[1].
Topoisomerase I inhibitor 17 inhibits DDX5 expression in HCT116 cells (100 nM, 48-72 h) and deregulates DDX5-blocked Top1 activity (5 and 50 μM) [1].

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

Topoisomerase I inhibitor 17 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HCT116
Concentration: 0, 2.5, 10, 50 nM
Incubation Time: 48 h
Result: Halted the progression of the G2/M checkpoint, resulted in a significant accumulation of cells at this critical pre-division stage, with increases in cell number observed at G2/M phases of 2.05% (0 nM), 33.48% (2.5 nM), 55.28% (5 nM) and 64.01% (10 nM), respectively.

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 50, 100 nM
Incubation Time: 72 h
Result: Reduced expression of anti-apoptotic proteins (e.g. Survivin).
Upregulated the pro-apoptotic proteins Bax and γH2AX in a dose-dependent manner.
In Vivo

Topoisomerase I inhibitor 17 (2-15 mg/kg, i.p., once a week for 4 weeks) effectively reduces human colon cancer PDX tumor mice tumors through concentration-dependent tumor suppression with acceptable toxicity[1]。

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

Animal Model: FL118 colorectal cancer (CRC) patient-derived xenograft (PDX) tumors models using a limited number of severe combined immunodeficiency (SCID) mice[1]
Dosage: 2, 8 and 15 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Regressed CRC PDX27454 tumors after 21 days with no recurrence within 35 days through a concentration-dependent tumor-suppressive effect and acceptable toxicity at 15 mg/kg.
Displayed stable mouse body weights.
Molecular Weight

516.47

Formula

C28H21FN2O7
CAS No.
SMILES

FC(C=CC(C1=C2C(C(N3C2)=CC([C@@](CC)4O)=C(C3=O)COC4=O)=NC5=CC6=C(C=C51)OCO6)=C7)=C7OC
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Topoisomerase I inhibitor 17 Related Classifications

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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.

Keywords:

Topoisomerase I inhibitor 172413582-45-1Topoisomerase I inhibitor17Topoisomerase I inhibitor-17TopoisomeraseReactive Oxygen SpeciesApoptosisSurvivinBcl-2 FamilyIAPDNA/RNA SynthesisAntitumorCytotoxicityHepG2Caco-2ProliferationMigrationPDXInhibitorinhibitorinhibit

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