2. Protein Tyrosine Kinase/RTK PROTAC
  3. FAK Ligands for Target Protein for PROTAC
  4. BI-4464

BI-4464 is a highly selective, ATP competitive PTK2/FAK protein kinase inhibitor with an IC50 value of 17 nM. BI-4464 can be used as a PTK2 ligand for constructing proteolysis targeting chimeras (PROTAC).

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BI-4464 Chemical Structure

BI-4464 Chemical Structure

CAS No. : 1227948-02-8

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BI-4464 Related Antibodies

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Description

BI-4464 is a highly selective, ATP competitive PTK2/FAK protein kinase inhibitor with an IC50 value of 17 nM. BI-4464 can be used as a PTK2 ligand for constructing proteolysis targeting chimeras (PROTAC).

IC50 & Target

IC50: 17 nM (PTK2/FAK)[1].
In Vitro

BI-4464 (0-10 μM, 18 h) inhibits human liver cancer cell proliferation by targeted degradation of PTK2 protein, with a pIC50 value of 5[1].
BI-4464 (0-20 μM, 48 h) has anti-Ebola potential by inhibiting aberrant endothelial cell (EC) activation through the inhibition of TNF-α and EBOV-like particles (VLP) -mediated up-regulation of ICAM-1[2].

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

BI-4464 Related Antibodies

Cell Proliferation Assay[1].

Cell Line: SNU387, HUH-1, Hep3B2.1-7, HepG2, SK-Hep-1 HLF, SNU-398, HUCCT1, HLE, HuH-7, SNU423 cell
Concentration: 0-10 μM
Incubation Time: 18 h
Result: Inhibited the proliferation of human hepatocellular carcinoma (HCC) cell lines with pIC50 values of approximately 5.

Cell Viability Assay[2].

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: 0-20 μM
Incubation Time: 48 h
Result: Showed potency in VLPs-treated ECs with an IC50 value of approximately 0.9 μM.
Molecular Weight

555.55

Formula

C28H28F3N5O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1CCN(C)CC1)C2=CC=C(NC3=NC=C(C(F)(F)F)C(OC4=CC=CC(CC5)=C4C5=O)=N3)C(OC)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (30.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8000 mL 9.0001 mL 18.0002 mL
5 mM 0.3600 mL 1.8000 mL 3.6000 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.64%

SDS (393 KB)

COA (249 KB) HNMR (150 KB) LCMS (107 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8000 mL 9.0001 mL 18.0002 mL 45.0005 mL
5 mM 0.3600 mL 1.8000 mL 3.6000 mL 9.0001 mL
10 mM 0.1800 mL 0.9000 mL 1.8000 mL 4.5000 mL
15 mM 0.1200 mL 0.6000 mL 1.2000 mL 3.0000 mL
20 mM 0.0900 mL 0.4500 mL 0.9000 mL 2.2500 mL
25 mM 0.0720 mL 0.3600 mL 0.7200 mL 1.8000 mL
30 mM 0.0600 mL 0.3000 mL 0.6000 mL 1.5000 mL
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BI-4464 Related Classifications

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:

BI-44641227948-02-8BI4464BI 4464FAKLigands for Target Protein for PROTACPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseTarget Protein-binding MoietyPROTACprotein degradationhepatocellular carcinoma cellInhibitorinhibitorinhibit

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