2. Protein Tyrosine Kinase/RTK Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. FAK Apoptosis Reactive Oxygen Species (ROS) Caspase
  4. 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.

FAK-IN-28 Chemical Structure

FAK-IN-28 Chemical Structure

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FAK-IN-28 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Caspase 3

 

In Vitro

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.

FAK-IN-28 Related Antibodies

Cell Migration Assay [1]

Cell Line: HCT116 cells
Concentration: 0.2 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 12 h, 24 h
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.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.2 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 25 μM
Incubation Time: 12 h, 24 h
Result: Enhanced caspase-3 activation and the number of apoptotic cell populations.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.2 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Increased G2/M cells and decreased the G0/G1 cell population.
In Vivo

FAK-IN-28 (Compound 10c) (50 mg/kg, p.o., once daily, 10 days) inhibits tumor growth and elicits no significant weight loss or hepatorenal toxicity in HCT116 xenograft nude mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HCT116 (5 × 106) xenograft female Balb/c nude mice model[1]
Dosage: 50 mg/kg
Administration: p.o., once daily, 10 days
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).
Molecular Weight

795.83

Formula

C37H40F3N9O6S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FAK-IN-28 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FAK-IN-28FAKApoptosisReactive Oxygen Species (ROS)CaspasePTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorHCT116 cellsHCT116 xenograftNude miceinhibitorinhibit

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