FAK-IN-29
FAK-IN-29 is a selective FAK inhibitor with an IC50 of 0.5 nM. FAK-IN-29 can inhibit the proliferation and colony formation of MDA-MB-231 cells, and induce cell cycle arrest and apoptosis. FAK-IN-29 exhibits antitumor activity and can be used for the research of tumors such as triple-negative breast cancer.
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- No. CAS: 3104566-26-6
- Fòrmula: C26H27FN8O2
- Peso molecular:502.54
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
FAK-IN-29 (Compound 7h) (3 μM; 24 h) induces G2/M phase cell cycle arrest in MDA-MB-231 cells[1].
FAK-IN-29 (0.15625-50 μM, 48 h) has IC50 values of 0.18, 0.17, and 0.15 μM against MDA-MB-231, SKOV3, and HepG2 cells, respectively[1].
FAK-IN-29 (0.3-3 μM; 24 h) induces concentration-dependent apoptosis in MDA-MB-231 cells[1].
FAK-IN-29 (0.3-3 μM; 24 h) significantly inhibits colony formation in MDA-MB-231 cells[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
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Concentration:3 μM
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Incubation Time:24 h
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Result:Caused a significant accumulation of MDA-MB-231 cells in the G2/M phase, with a corresponding decrease in the G0/G1 phase. The G2/M phase population increased from 10.4% to 35.7%, while the G0/G1 phase decreased from 68.3% to 45.2%.
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Cell Line:MDA-MB-231
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Concentration:0.3, 1, and 3 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a concentration-dependent manner. The total apoptotic rates were 5.62 %, 33.15 %, and 62.48 % at concentrations of 0.3, 1, and 3 μM, respectively.
In Vivo
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 tumor xenograft model)[1]
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Dosage:5 mg/kg, 10 mg/kg
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Administration:i.v.
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Result:Achieved 61.8% tumor growth inhibition in MDA-MB-231 xenograft models, comparable to Paclitaxel (HY-B0015) (54.8%) at 10 mg/kg.
Significantly reduced Tumor volumes in both 5 mg/kg and 10 mg/kg groups.
Caused no observable toxicity, and body weights and organ weights remained stable.
Caused no histopathological abnormalities.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Soft Agar Colony Formation Assay
- Colony Formation (Clonogenic) Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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No. CAS 3104566-26-6
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Peso molecular 502.54
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Fòrmula C26H27FN8O2
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SMILES
O=C(NC)C1=CC=CC=C1NC2=C3C(NC=C3F)=NC(NC4=CC=CC(CC(N5CCNCC5)=O)=C4)=N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FAK-IN-29 Related Classifications
HY-179679 Related Classifications
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