FAK-IN-28
FAK-IN-28 is an orally active FAK inhibitor (IC50 = 0.4 nM). FAK-IN-28 exhibits dual antiproliferative and anti-metastatic properties. FAK-IN-28 triggers caspase-3-dependent apoptosis via ROS elevation. FAK-IN-28 inhibits tumor growth without causing weight loss or hepatotoxicity. FAK-IN-28 is useful in the study of FAK-driven malignancies, such as colon cancer, cervical cancer, triple-negative breast cancer, and melanoma.
For research use only. We do not sell to patients.
- Formula: C37H40F3N9O6S
- Molecular Weight:795.83
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Caspase 3 |
FAK-IN-28 (Compound 10c) (12 h) shows cytotoxic effects on HCT116, HeLa, MDA-MB-231 and A375 cells, with IC50s of 0.08, 0.31, 0.23, 0.29 μM, respectively[1].
FAK-IN-28 (0.2-25 μM, 1-24 h) inhibits cell invasion and reduces the number of adhered cells in HCT116 cells[1].
FAK-IN-28 (0.2-25 μM, 12-24 h) enhances caspase-3 activation and the number of apoptotic cell populations, disrupts cell cycle progression in HCT116 cells[1].
FAK-IN-28 (1-125 μM, 12 h) exhibits ROS-inducing activity in HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:0.2 μM, 0.5 μM, 1 μM, 2 μM
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Incubation Time:12 h, 24 h
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Result:Inhibited cell invasion at 0.5 μM and enhanced inhibition at 2 μM, which was superior to TAE226 (HY-13203) at the same concentration.
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Cell Line:HCT116 cells
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Concentration:0.2 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 25 μM
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Incubation Time:12 h, 24 h
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Result:Enhanced caspase-3 activation and the number of apoptotic cell populations.
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Cell Line:HCT116 cells
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Concentration:0.2 μM, 0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Increased G2/M cells and decreased the G0/G1 cell population.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCT116 (5 × 106) xenograft female Balb/c nude mice model[1]
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Dosage:50 mg/kg
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Administration:p.o., once daily, 10 days
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Result:Inhibited tumor growth by 62.22% (TAE226 group was 50.98%).
Did not change body weight, kept serum biochemical parameters (ALT, AST, ALP, LDH) within normal range, and did not cause pathological changes (necrosis, inflammation or fibrosis).
Chemical Information
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Molecular Weight 795.83
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Formula C37H40F3N9O6S
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SMILES
COC1=CC(N2CCN(C(C3=CC=CC(S(=O)(N4CCN(C(C)=O)CC4)=O)=C3)=O)CC2)=CC=C1NC5=NC(NC6=C(C(NC)=O)C=CC=C6)=C(C(F)(F)F)C=N5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FAK-IN-28 Related Classifications
HY-175039 Related Classifications
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