FAK-IN-26
FAK-IN-26 is a BBB-penetrable Focal Adhesion Kinase (FAK) inhibitor (IC50: 0.87 nM). FAK-IN-26 significantly suppresses tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 has potent anti-cancer activity in A549 and SKOV-3 tumor mice models with tumor inhibition rates of 59.15 % and 57.9 %.
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- CAS No.: 2801785-12-4
- Formule: C20H19BrFN5O2
- Masse moléculaire:460.30
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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- Références
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Help & FAQs
Activité biologique
0.87 nM
FAK-IN-26 (Compound A8) has superior binding capacity on FAK with a Kd of 15 μM[1].
FAK-IN-26 (1 μmol/L) has broad-spectrum inhibitory activity against multiple kinases, with FAK and FYNα being inhibited by more than 95 %[1].
FAK-IN-26 (0.5-10 μM) significantly reduces the viability of A549 and SKOV-3 cells at lower concentrations compared to Defactinib (VS6063) (HY-12289).
FAK-IN-26 (0.2-1.6 μM) dose-dependently reduces the cancer stem cell population in A549 and SKOV-3 cells[1].
FAK-IN-26 (62.5-1000 nM, 72 h) significantly induces G2/M arrest in both A549 and SKOV-3 cell lines[1].
FAK-IN-26 (0.1-10 nM, 6-48 h) dose-dependently decreases migration rates and distances of A549 and SKOV-3 cells with significant inhibition observed at concentrations of 1 nM and 10 nM[1].
FAK-IN-26 (31.25-62.5 nM, 48 h) effectively inhibits FAK autophosphorylation in both A549 and SKOV-3 cells in a dose-dependent manner, with greater efficacy in A549 cells[1].
FAK-IN-26 has favorable metabolic stability in human liver microsomes with CLint and T1/2 of 31.8 μL/min/mg and 43.6 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells, SKOV-3 cells
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Concentration:62.5, 125, 250, 500, 1000 nM
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Incubation Time:72 h
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Result:Significantly arrested A549 cells and SKOV-3 cells in the G2/M phase, and the proportion of A549 cells were 70.8 %, 68.7 %, 68.8 %, 57.9 %, and 44.7 %, respectively.
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Cell Line:A549 cells, SKOV-3 cells
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Concentration:0.1, 1, 10 nM
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Incubation Time:6, 12, 24, 48 h
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Result:Dose-dependently decreased migration rates and distances of A549 and SKOV-3 cells with significant inhibition observed at concentrations of 1 nM and 10 nM.
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Cell Line:A549 cells, SKOV-3 cells
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Concentration:31.25, 62.5 nM
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Incubation Time:48 h
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Result:Effectively inhibited the protein expression of p-FAK925 in both A549 and SKOV-3 cells in a dose-dependent manner, with greater efficacy in A549 cells.
FAK-IN-26 (500-2000 mg/kg) is well-tolerated up to 2000 mg/kg in mice without causing acute toxicity[1].
FAK-IN-26 has favorable tumor uptake and retention, with a peak uptake of 4.16 ID/g at 30 min post-injection in S180 tumor-bearing mice and efficiently penetrates the BBB, with brain uptake of 2.63 % ID/g at 15 min and 1.62 % ID/g at 120 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Kunming mice were injected subcutaneously with A549 and KOV-3 cells until tumor volume reached 70-100 mm3[1].
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Dosage:A549 tumor model: 50 mg/kg, SKOV-3 tumor model: 25 mg/kg
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Administration:oral gavage (p.o.), once a day for five days followed by two days off (A549 tumor model), twice daily for five days followed by two days off (SKOV-3 tumor model), and then measures tumor volume and weight.
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Result:Significantly increased tumor inhibition rate of 59.15 %, superior to VS6063 and Erlotinib with tumor inhibition rate of 40.69 % and 47.41 % in the A549 tumor model.
Achieved tumor inhibition rate of 57.9 %, superior to VS6063 and Paclitaxel with tumor inhibition rate of 53.89 % and 55.30 %, and the combination therapy with Paclitaxel further enhanced anti-tumor effects (tumor inhibition rate: 76.63 %) in the SKOV-3 tumor model.
Chemical Information
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CAS No. 2801785-12-4
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Masse moléculaire 460.30
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Formule C20H19BrFN5O2
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SMILES
O=C(NC)C1=CC=CC=C1NC2=NC(NC3=CC=C(OCCF)C=C3)=NC=C2Br
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FAK-IN-26 Related Classifications
HY-173515 Related Classifications
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