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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.23%
- 分子式: C22H20ClN7
- 分子量:417.89
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
製品説明
体外実験
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.
体内実験
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.
化学情報
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性状 Solid
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分子量 417.89
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ZSTK3744 関連分類
HY-181629A 関連分類
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