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Cat. No.: HY-187711

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FAK-IN-33

FAK-IN-33 is a potent focal adhesion kinase (FAK) inhibitor with an IC₅₀ value of 10.23 nM against FAK. FAK-IN-33 inhibits the viability of U118-MG glioblastoma cells with an IC₅₀ of 0.29 μM, and shows low cytotoxicity toward LO2 and 2BS cells. FAK-IN-33 can be used in studies related to glioblastoma.

For research use only. We do not sell to patients.

Formula: C₂₄H₂₁F₃N₆O₂
Molecular Weight:482.46

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

FAK-IN-33 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target

^[1]

FAK

10.23 nM (IC₅₀)

In Vitro

Anti-cancerOthersApoptosisCell Cycle Regulation

Anti-cancer

FAK-IN-33 (compound 5f) (0.005-50 μM; 72 h) potently inhibits the proliferation of U118-MG glioblastoma cells, with an IC₅₀ of 0.29 μM^[1].
FAK-IN-33 (72 h) exhibits low toxicity to LO2 normal hepatocytes (IC₅₀ = 7.12 μM) and 2BS normal fibroblasts (IC₅₀ = 32.10 μM), demonstrating selective activity against tumor cells^[1].

Others

FAK-IN-33 potently inhibits purified FAK kinase with an IC₅₀ of 10.23 nM^[1].
FAK-IN-33 exhibits stronger binding affinity to FAK kinase (PDB ID: 2JKK) than TAE-226, forms an additional hydrogen bond with Glu502, and has a shorter binding distance^[1].

Anti-cancer

Apoptosis

FAK-IN-33 (0.04-2 μM) induces apoptosis in U118-MG cells in a concentration-dependent manner; at 2 μM, the proportion of late apoptotic cells increases from 2.54% in the control group to 16.5%, and the proportion of total apoptotic cells is approximately twice that of the TAE-226 group at the same concentration^[1].

Anti-cancer

Cell Cycle Regulation

FAK-IN-33 (0.2-0.8 μM; 24 h) induces G2/M phase arrest in U118-MG cells; the proportion of cells in G2/M phase increases from 7.84% in the control group to 68.61% at 0.2 μM and 78.09% at 0.8 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

U118-MG glioblastoma cells
Concentration:

0.005-50 μM
Incubation Time:

72 h
Result:

Inhibited proliferation of U118-MG cells with an IC₅₀ of 0.29 μM, which was 12-fold more potent than the positive control TAE-226 (IC₅₀ = 3.69 μM).

Cell Cycle Analysis^[1]

Cell Line:

U118-MG glioblastoma cells
Concentration:

MG0.2, 0.4, 0.8 μM
Incubation Time:

24 h
Result:

Induced cell cycle arrest at the G2/M phase in U118-MG cells.
At 0.2 μM, the proportion of G2/M phase cells increased to 68.61% (from 7.84% in untreated controls); at 0.8 μM, the proportion further increased to 78.09%, which was significantly higher than the effect of TAE-226 at the same concentration.

Related Protocols :

Chemical Information

Molecular Weight 482.46
Formula C₂₄H₂₁F₃N₆O₂
SMILES

O=C(NC)C1=CC=CC=C1NC2=C(C(F)(F)F)C=NC(NC3=CC(/C(C(N4)=O)=C/CC)=C4C=C3)=N2
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

Handling Instructions (2659 KB)

References

[1]. Tan Y, et al. Synthesis and Biological Evaluation of Diaminopyrimidine Derivatives as FAK Inhibitors With Anti-glioblastoma Activity. ChemistrySelect. 2026;11:e73946.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
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- In Vitro
Chemical Information
Purity & Documentation
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FAK-IN-33

Biological Activity

Description

IC50 & Target

In Vitro

Chemical Information

Purity & Documentation

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