ZSTK3744 free base
ZSTK3744 free base is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 free base directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 free base induces apoptosis in triple-negative breast cancer cells. ZSTK3744 free base exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.
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- CAS No.: 3106975-38-3
- Formule: C22H19N7
- Masse moléculaire:381.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
ZSTK3744 free base (0.1-1000 nM; 72 h) (compound 12) potently inhibits the growth of MDA-MB-468 triple-negative breast cancer (TNBC) cells, with an IC50 of 0.87 nM[1].
ZSTK3744 free base (0.1-1000 nM; 72 h) potently inhibits the growth of Doxorubicin (HY-15142A)-resistant MDA-MB-468/AR triple-negative breast cancer (TNBC) cells, with an IC50 of 0.92 nM[1].
ZSTK3744 free base (0.1-1000 nM; 72 h) inhibits the growth of Paclitaxel (HY-B0015)-resistant MDA-MB-468/PR triple-negative breast cancer (TNBC) cells with an IC50 of 23.54 nM[1].
ZSTK3744 free base (1-24 h) upregulates the mRNA expression of CYP1A1 and TIPARP in MDA-MB-468 triple-negative breast cancer (TNBC) cells in a time-dependent manner, with significant induction observable as early as 1 hour after treatment[1].
ZSTK3744 free base (24 h) induces apoptosis in MDA-MB-468 TNBC cells, and its cell growth inhibitory activity is mediated at least partially via the caspase-dependent apoptotic pathway[1].
ZSTK3744 free base (0.1-1000 nM; 72 h) potently inhibits the growth of MDA-MB-453 triple-negative breast cancer (TNBC) cells, with an IC50 of 1.14 nM[1].
ZSTK3744 free base (0.1-1000 nM; 72 h) potently inhibits the growth of DU4475 triple-negative breast cancer (TNBC) cells, with an IC50 of less than 0.50 nM[1].
ZSTK3744 free base (0.1-1000 nM; 72 h) exerts no significant inhibitory effect on the growth of Hs578T TNBC cells, with an IC50 >500 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-453 TNBC cells
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Concentration:0.1, 1, 10, 100 and 10,000 nM
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Incubation Time:72 h
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Result:Inhibited cell growth with an IC50 of 1.14 nM.
In Vivo
ZSTK3744 free base (1-5 mg/kg; i.v.; on days 0, 4, and 8) inhibits tumor growth in parental triple-negative breast cancer (TNBC) mouse xenograft models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.CB17-Prkdcscid/J (NOD/SCID) (female, 6 weeks old, subcutaneous xenograft of Doxorubicin-resistant MDA-MB-468 cells)[1]
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Dosage:2.5 mg/kg; 10 mg/kg
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Administration:i.v.; on days 0, 7, and 14
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Result:Inhibited tumor growth in a dose-dependent manner.
Reduced tumor volume significantly compared with the vehicle-treated group and the eribulin-treated group.
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Animal Model:NOD.CB17-Prkdcscid/J (NOD/SCID) (female, 6 weeks old, subcutaneous xenograft of parental MDA-MB-468 cells)[1]
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Dosage:1 mg/kg; 2.5 mg/kg; 5 mg/kg
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Administration:i.v.; on days 0, 4, and 8
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Result:Reduced tumor volume at 2.5 and 5 mg/kg.
Reduced tumor volume relative to the vehicle-treated group at all tested doses, with the highest dose showing the greatest inhibition.
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Protocol for Cell Counting and Cell Density Analysis
- Somatic Cell Culture
- Apoptosis Solutions
- CCK-8/WST-8 Cell Proliferation Assay
- Cell Counting-Based Growth Curve Assay
- MTT Cell Proliferation Assay
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 3106975-38-3
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Masse moléculaire 381.43
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Formule C22H19N7
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SMILES
CC1=CC=CC2=C1N=CN2C3=NC(C4=CC(CCN5)=C5N=C4)=C(C=CN6C)C6=N3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZSTK3744 free base Related Classifications
HY-181629 Related Classifications
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