ZSTK3744
Based on 1 Customer Validation
ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 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 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.
For research use only. We do not sell to patients.
- Purity: 98.23%
- Formula: C22H20ClN7
- Molecular Weight:417.89
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
In Vitro
ZSTK3744 (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 (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 (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 (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 (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 (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 (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 (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 (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.; days 0, 7, 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.
Caused no significant effect on mouse body weight.
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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.; days 0, 4, 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.
Chemical Information
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Appearance Solid
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Molecular Weight 417.89
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Formula C22H20ClN7
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Color Light yellow to yellow
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SMILES
CC1=CC=CC2=C1N=CN2C3=NC(C4=CC(CCN5)=C5N=C4)=C(C=CN6C)C6=N3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Purity & Documentation
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Data Sheet (290 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZSTK3744 Related Classifications
HY-181629A Related Classifications
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