2. Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease
  3. Aryl Hydrocarbon Receptor Apoptosis Caspase Cytochrome P450
  4. ZSTK3744 hydrochloride

ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride 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 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.

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ZSTK3744 hydrochloride

ZSTK3744 hydrochloride Chemical Structure

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ZSTK3744 hydrochloride Related Antibodies

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Description

ZSTK3744 hydrochloride is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 hydrochloride 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 hydrochloride induces apoptosis in triple-negative breast cancer cells. ZSTK3744 hydrochloride exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer[1].

In Vitro

ZSTK3744 (0.1-1000 nM; 72 h) (compound 12) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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) hydrochloride 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.

ZSTK3744 hydrochloride Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-453 TNBC cells
Concentration: 0.1, 1, 10, 100 and 10,000 nM
Incubation Time: 72 h
Result: Inhibited cell growth with an IC50 of 1.14 nM.
In Vivo

ZSTK3744 (2.5-10 mg/kg; i.v.; on days 0, 7, and 14) hydrochloride exerts significant, dose-dependent tumor growth inhibition effects in a Doxorubicin (HY-15142A)-resistant triple-negative breast cancer (TNBC) mouse xenograft model[1].
ZSTK3744 (1-5 mg/kg; i.v.; on days 0, 4, and 8) hydrochloride 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.

Animal Model: NOD.CB17-Prkdcscid/J (NOD/SCID) (female, 6 weeks old, subcutaneous xenograft of Doxorubicin-resistant MDA-MB-468 cells)[1]
Dosage: 2.5 mg/kg; 10 mg/kg
Administration: i.v.; days 0, 7, 14
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.
Animal Model: NOD.CB17-Prkdcscid/J (NOD/SCID) (female, 6 weeks old, subcutaneous xenograft of parental MDA-MB-468 cells)[1]
Dosage: 1 mg/kg; 2.5 mg/kg; 5 mg/kg
Administration: i.v.; days 0, 4, 8
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.
Molecular Weight

417.89

Formula

C22H20ClN7
SMILES

CC1=CC=CC2=C1N=CN2C3=NC(C4=CC(CCN5)=C5N=C4)=C(C=CN6C)C6=N3.Cl
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
References
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ZSTK3744 hydrochloride Related Classifications

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Help & FAQs
  • 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:

ZSTK3744ZSTK 3744ZSTK-3744Aryl Hydrocarbon ReceptorApoptosisCaspaseCytochrome P450AhRCYPstriple-negative breast cancer cellspan-caspase inhibitorABCB1CYP1B1mouse xenograft modelshuman precision-cut lung slicesTIPARPCYP1A1Inhibitorinhibitorinhibit

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