1. Protein Tyrosine Kinase/RTK
  2. FAK
  3. 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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FAK-IN-9 Chemical Structure

FAK-IN-9 Chemical Structure

CAS No. : 2911655-93-9

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Description

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[1].

IC50 & Target

IC50: 27.44 nM (FAK)[1]

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-157, MDA-MB-231, MDA-MB-453 and MCF10A
Concentration:
Incubation Time: 72 h
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.

Cell Invasion Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 1, 2 and 4 μM
Incubation Time: 48 h
Result: The numbers of invasive MDA-MB-231 cells were reduced dose-dependently.

Cell Migration Assay [1]

Cell Line: MDA-MB-231 cells
Concentration: 1, 2 and 4 μM
Incubation Time: 48 h
Result: Remarkably block the migration of MDA-MB-231 cells in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1, 2 and 4 μM
Incubation Time: 72 h
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.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 1, 2 and 4 μM
Incubation Time: 72 h
Result: The percentage of apoptotic MDA-MB-231 cells gradually increased ranging from 19.06% to 77.66% at 4 μM.
In Vivo

FAK-IN-9 (Compound 8f; 15 or 30 mg/kg; oral; once daily for 30 days) inhibits MDA-MB-231 lung metastasis in mice[1].

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

Animal Model: BALB/c nude mice, MDA-MB-231 experimental pulmonary metastasis model[1]
Dosage: 15 or 30 mg/kg
Administration: Oral, once daily for 30 days
Result: Potently reduced the numbers of lung tumor nodules dose-dependently.
Molecular Weight

764.25

Formula

C36H38ClN7O8S

CAS No.
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

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-9 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.

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FAK-IN-9
Cat. No.:
HY-149259
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