BI-4464
Based on 1 Customer Validation
BI-4464 is a highly selective, ATP competitive PTK2/FAK protein kinase inhibitor with an IC50 value of 17 nM. BI-4464 is a FAK (HY-43760) ligand and linker conjugate. BI-4464 can be used to construct proteolysis targeting chimeras (PROTACs), such as PROTAC FAK degrader 4 (HY-178467). PROTAC FAK degrader 4 is a highly potent and selective FAK PROTAC degrader.
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- Purity: 98.64%
- CAS No.: 1227948-02-8
- 화학식: C28H28F3N5O4
- 분자량:555.55
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
IC50: 17 nM (PTK2/FAK)[1].
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.
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Cell Line:SNU387, HUH-1, Hep3B2.1-7, HepG2, SK-Hep-1 HLF, SNU-398, HUCCT1, HLE, HuH-7, SNU423 cell
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Concentration:0-10 μM
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Incubation Time:18 h
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Result:Inhibited the proliferation of human hepatocellular carcinoma (HCC) cell lines with pIC50 values of approximately 5.
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Cell Line:Human umbilical vein endothelial cells (HUVECs)
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Concentration:0-20 μM
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Incubation Time:48 h
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Result:Showed potency in VLPs-treated ECs with an IC50 value of approximately 0.9 μM.
Chemical Information
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CAS No. 1227948-02-8
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Appearance Solid
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분자량 555.55
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화학식 C28H28F3N5O4
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Color Light yellow to yellow
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Popow J, et al. Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions. J Med Chem. 2019 Mar 14;62(5):2508-2520. [Content Brief]
[2]. Moni BM, et al. Ebola Virus GP Activates Endothelial Cells via Host Cytoskeletal Signaling Factors. Viruses. 2022 Jan 13;14(1):142. [Content Brief]
[3]. Liu C, et al. Structure-guided design of a potent focal adhesion kinase (FAK) degrader via ternary complex modeling and molecular dynamics simulation. Bioorg Chem. 2025 Oct;165:109017. [Content Brief]
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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