FAK-IN-9
FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis.
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- CAS 番号: 2911655-93-9
- 分子式: C36H38ClN7O8S
- 分子量:764.25
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Help & FAQs
生物活性
IC50: 27.44 nM (FAK)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF-10A | IC50 |
2.401 μM
Compound: 8f
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Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 36801517] |
| MDA-MB-157 | IC50 |
0.167 μM
Compound: 8f
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Antiproliferative activity against human MDA-MB-157 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-157 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 36801517] |
| MDA-MB-231 | IC50 |
0.126 μM
Compound: 8f
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 36801517] |
| MDA-MB-453 | IC50 |
0.159 μM
Compound: 8f
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Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 36801517] |
FAK-IN-9 (Compound 8f; 72 h) shows antiproliferative activity with IC50s of 0.167±0.025, 0.126±0.012 and 0.159±0.017 μM against MDA-MB-157, MDA-MB-231 and MDA-MB-453 cells, respectively[1].
FAK-IN-9 (1-4 μM; 72 h) leads to relatively high levels of NO production in a dose-dependent manner in MDA-MB-231 cells[1].
FAK-IN-9 (1-4 μM; 48 h) inhibits invasion and migration of MDA-MB-231 cells[1].
FAK-IN-9 (1-4 μM; 72 h) efficiently blocks FAK mediated-signaling pathways[1].
FAK-IN-9 (4 μM; 72 h) inhibits the formation of focal adhesions (FAs) and stress fibers (SFs) in MDA-MB-231 cells[1].
FAK-IN-9 (1-4 μM; 72 h) induces MDA-MB-231 cell apoptosis[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-157, MDA-MB-231, MDA-MB-453 and MCF10A
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Concentration:
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Incubation Time:72 h
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Result:Inhibited proliferation with IC50s of 0.167±0.025, 0.126±0.012, 0.159±0.017 and 2.401±0.131 μM against MDA-MB-157, MDA-MB-231, MDA-MB-453 and MCF10A, respectively.
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Cell Line:MDA-MB-231 cells
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Concentration:1, 2 and 4 μM
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Incubation Time:48 h
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Result:The numbers of invasive MDA-MB-231 cells were reduced dose-dependently.
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Cell Line:MDA-MB-231 cells
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Concentration:1, 2 and 4 μM
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Incubation Time:48 h
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Result:Remarkably block the migration of MDA-MB-231 cells in a dose-dependent manner.
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Cell Line:MDA-MB-231 cells
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Concentration:1, 2 and 4 μM
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Incubation Time:72 h
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Result:Potently suppressed the autophosphorylation of Y397 in a dose-dependent manner. Decreased the levels of p-AKT, MMP-2 and MMP-9 dose dependently.
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Cell Line:MDA-MB-231 cells
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Concentration:1, 2 and 4 μM
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Incubation Time:72 h
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Result:The percentage of apoptotic MDA-MB-231 cells gradually increased ranging from 19.06% to 77.66% at 4 μM.
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, MDA-MB-231 experimental pulmonary metastasis model[1]
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Dosage:15 or 30 mg/kg
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Administration:Oral, once daily for 30 days
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Result:Potently reduced the numbers of lung tumor nodules dose-dependently.
化学情報
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CAS 番号 2911655-93-9
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分子量 764.25
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分子式 C36H38ClN7O8S
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SMILES
CNC(C1=C(C=CC=C1)NC2=C(C=NC(NC3=CC=C(C=C3)CC(OCCCCCCCCOC4=NO[N+]([O-])=C4S(=O)(C5=CC=CC=C5)=O)=O)=N2)Cl)=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)
FAK-IN-9 関連分類
HY-149259 関連分類
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