STAT3/CAIX-IN-1
STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC).
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- CAS 番号: 3053583-60-8
- 分子式: C28H23F6N5O5S2
- 分子量:687.63
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
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CA IX 80.45 nM (IC50) |
hCA VB 25.40 nM (IC50) |
hCA II 349.30 nM (IC50) |
STAT3 60.03 μM (Kd) |
STAT3/CAIX-IN-1 (Compound 7m) (2-8 μM, 24 h) inhibits STAT3 phosphorylation in MDA-MB-231 cells[1].
STAT3/CAIX-IN-1 (4 μM) binds to STAT3 to enhance its stability[1]. STAT3/CAIX-IN-1 enhances proliferation inhibition of tumor cell lines with IC50s of 2.18 μM (hypoxia) and 4.21μM (normoxia) in the MDA-MB-231 cell line[1].
STAT3/CAIX-IN-1 (4 μM, 8 μM, 24 h) induces ferroptosis via the GPX4 pathway, increases reactive oxygen species (ROS) levels, upregulates intracellular lipid peroxidation in MDA-MB-231 cells[1].
STAT3/CAIX-IN-1 (2 μM, 4 μM, 24-48 h) inhibits the migration of MDA-MB-231 cells[1]. STAT3/CAIX-IN-1 (4 μM, 8 μM, 24 h) induces apoptosis in MDA-MB-231 cells, induces cell cycle arrest in MDA-MB-231 cells at the G1/S phase[1].
STAT3/CAIX-IN-1 has anti-tumor activity with IC50s of 4.21 μM (MDA-MB-231), 5.67 μM (MCF-7), 6.60 μM (MDA-MB-231/ADR), 14.19 μM (MCF-10A)[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-231 cells
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Concentration:2, 4, 8 μM
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Incubation Time:24 h
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Result:Inhibited the levels of pSTAT3-S727 and pSTAT3-Y705.
No changed p-JAK1 levels.
Reduced GPX4 levels.
Downregulated the expression of Bcl-2 and Cyclin D1.
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Cell Line:MDA-MB-231 cells
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Concentration:4, 8 μM
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Incubation Time:24 h
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Result:Accumulated in G1 phase cells, downregulated S phase cells.
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Cell Line:MDA-MB-231 cells
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Concentration:4, 8 μM
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Incubation Time:24 h
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Result:Induced apoptosis in MDA-MB-231 cells.
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Cell Line:MDA-MB-231 cells
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Concentration:2, 4, 8 μM
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Incubation Time:24 h, 48 h
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Result:Reduced mobility.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | F | C0 | Vss | Vz | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 5.63 h | 1.00 h | 190.74 ng/mL | 1046.58 ng·h/mL | 1093.83 ng·h/mL | 5.66 h | 6.79 h | 64.70 % | / | / | / | / |
| Mice[1] | 2 mg/kg | i.v. | 9.42 h | 0.08 h | 211.2 ng/mL | 323.52 ng·h/mL | 380.54 ng·h/mL | 5.84 h | 10.49 h | / | 342.31 ng/mL | 54013.50 mL/kg | 70742.38 mL/kg | 5344.57 mL/h/kg |
STAT3/CAIX-IN-1 (Compound 7m) (5 mg/kg, 10 mg/kg, 48 h) shows anti-tumor activity with 75% TIR, not changes weight or behavior[1].
STAT3/CAIX-IN-1 (10 mg/kg, i.p.,21 days, every 2 days) reduces phosphorylated STAT3 expression in Balb/c nude mouse xenograft experiments[1].
STAT3/CAIX-IN-1 (5 mg/kg, 10 mg/kg, i.p., 21 days, every 2 days) inhibits tumor growth on Balb/c nude mice with MDA-MB-231 xenograft tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c nude mice with MDA-MB-231 xenograft tumors[1].
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Dosage:10 mg/kg
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Administration:i.p.,21 days, every 2 days
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Result:Reduced the fluorescence intensity of pSTAT3-S727 (green fluorescence) and pSTAT3-Y705 (red fluorescence).
化学情報
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CAS 番号 3053583-60-8
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分子量 687.63
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分子式 C28H23F6N5O5S2
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SMILES
O=C(NC1=NN=C(S(=O)(N)=O)S1)CCCC(N2C/C(C(/C(C2)=C/C3=CC=C(C(F)(F)F)C=C3)=O)=C\C4=CC=C(C(F)(F)F)C=C4)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
STAT3/CAIX-IN-1 関連分類
HY-174457 関連分類
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