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BI-4464

Name: BI-4464
Brand: TargetMol
SKU: T5480
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5480Cas No. 1227948-02-8

BI-4464, a highly selective ATP-competitive inhibitor of PTK2/FAK, exhibits an IC50 of 17 nM and serves as a PTK2 ligand for PROTAC (Proteolysis Targeting Chimera).

BI-4464

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Purity: 99.81%

Catalog No. T5480Cas No. 1227948-02-8

BI-4464, a highly selective ATP-competitive inhibitor of PTK2/FAK, exhibits an IC50 of 17 nM and serves as a PTK2 ligand for PROTAC (Proteolysis Targeting Chimera).

Pack Size	Price	USA Warehouse	Global Warehouse
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

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.81%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

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

Description	BI-4464, a highly selective ATP-competitive inhibitor of PTK2/FAK, exhibits an IC50 of 17 nM and serves as a PTK2 ligand for PROTAC (Proteolysis Targeting Chimera).
Targets&IC50	PTK2/FAK:17 nM

Chemical Properties

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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	1.8000 mL	9.0001 mL	18.0002 mL	90.0009 mL
5 mM	0.3600 mL	1.8000 mL	3.6000 mL	18.0002 mL
10 mM	0.1800 mL	0.9000 mL	1.8000 mL	9.0001 mL
20 mM	0.0900 mL	0.4500 mL	0.9000 mL	4.5000 mL

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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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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