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BI-4464
Catalog No. T5480 Copy Product Info
Purity: 99.81%
🥰Excellent
BI-4464 is a highly selective inhibitor targeting focal adhesion kinase (FAK). BI-4464 effectively blocks the catalytic activity of FAK by competitively binding to the ATP-binding site, with an IC₅₀ of 17 nM. In addition to its role as a kinase inhibitor, BI-4464 can also serve as a FAK-targeting ligand (warhead) for PROTAC design. By conjugation with an E3 ligase ligand via an appropriate linker, the resulting PROTAC molecule can induce the selective degradation of FAK through the ubiquitin–proteasome pathway, providing a valuable tool for cancer biology and related disease research.
BI-4464
Copy Product Info🥰Excellent
Catalog No. T5480
BI-4464 is a highly selective inhibitor targeting focal adhesion kinase (FAK). BI-4464 effectively blocks the catalytic activity of FAK by competitively binding to the ATP-binding site, with an IC₅₀ of 17 nM. In addition to its role as a kinase inhibitor, BI-4464 can also serve as a FAK-targeting ligand (warhead) for PROTAC design. By conjugation with an E3 ligase ligand via an appropriate linker, the resulting PROTAC molecule can induce the selective degradation of FAK through the ubiquitin–proteasome pathway, providing a valuable tool for cancer biology and related disease research.
Cas No. 1227948-02-8
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| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $31 | In Stock | In Stock | |
| 5 mg | $74 | In Stock | In Stock | |
| 10 mg | $118 | In Stock | In Stock | |
| 25 mg | $213 | In Stock | In Stock | |
| 50 mg | $322 | In Stock | In Stock | |
| 100 mg | $449 | In Stock | In Stock | |
| 200 mg | $633 | - | In Stock |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
Batch Information
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Purity:99.81%
Appearance:Solid
Color:White
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Product Introduction
BI-4464 AI Summary
BI-4464 inhibits the PTK2 enzyme activity with an IC50 value of 2.0 nM, as evidenced by an Enzyme Assay measuring the phosphorylation of a specific substrate using a DELFIA assay. It displays strong antiproliferative activity across various human cell lines, with IC50 values ranging from 3162.28 to 7943.28 nM after six days of incubation. This compound also shows potent inhibition of human PTK2 (residues 411-689) expressed in Hi-5 cells, achieving IC50 values of 15.85 nM and 17.0 nM. Additionally, it induces PTK2 degradation in human A549 cells, with a pDC50 value greater than 10000.0. The thermodynamic solubility of BI-4464 in a phosphate buffer at pH 7 is approximately Log S = -4.19 after one hour of incubation, indicating high solubility under these conditions..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | BI-4464 is a highly selective inhibitor targeting focal adhesion kinase (FAK). BI-4464 effectively blocks the catalytic activity of FAK by competitively binding to the ATP-binding site, with an IC₅₀ of 17 nM. In addition to its role as a kinase inhibitor, BI-4464 can also serve as a FAK-targeting ligand (warhead) for PROTAC design. By conjugation with an E3 ligase ligand via an appropriate linker, the resulting PROTAC molecule can induce the selective degradation of FAK through the ubiquitin–proteasome pathway, providing a valuable tool for cancer biology and related disease research. |
| Targets&IC50 | PTK2/FAK:17 nM |
| Molecular Weight | 555.55 |
| Formula | C28H28F3N5O4 |
| Cas No. | 1227948-02-8 |
| Smiles | O(C1=C2C(CCC2=O)=CC=C1)C=3C(C(F)(F)F)=CN=C(NC4=C(OC)C=C(C(NC5CCN(C)CC5)=O)C=C4)N3 |
| Relative Density. | 1.41 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 16.67 mg/mL (30.01 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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