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Art. -Nr.: HY-158248

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FGFR4-IN-19

FGFR4-IN-19 (compound 8B) is a potent covalent fibroblast growth factor receptor 4 (FGFR4) inhibitor (IC₅₀=1.2 nM). FGFR4-IN-19 achieves high efficiency and isotype selectivity by covalently targeting a rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 can be used for hepatocellular carcinoma (HCC) research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3036751-84-2
Formel: C₂₁H₁₄Cl₃N₅O₄
Molecular Weight:506.73

Speicherung:

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

Data Sheet (273 KB)

FGFR4-IN-19 Chemical Structure

CAS. Nr.: 3036751-84-2

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

FGFR4

1.2 nM (IC₅₀)

FGFR1

4370 nM (IC₅₀)

FGFR2

490 nM (IC₅₀)

FGFR3

>5000 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Hep 3B2	EC₅₀	22 nM Compound: 8B	Antiproliferative activity against human Hep3B cells measured after 4 days by Celltiter-glo based luminescent assay Antiproliferative activity against human Hep3B cells measured after 4 days by Celltiter-glo based luminescent assay	[PMID: 38604131]

In Vitro

FGFR4-IN-19 shows weak inhibitory activity for FGFR1 (IC₅₀=4.4 μM) and FGFR2 (IC₅₀=490 nM), while all other IC₅₀ values were above 5 μM. FGFR4-IN-19 has highly selective within the FGFR family^[1].
FGFR4-IN-19 shows potent cellular FGFR4 engagement (EC₅₀=52±7 nM) compared to the FGFR1-3 (EC₅₀＞10 μM)^[1].
FGFR4-IN-19 (0.3 μM, 24 h) shows good antiproliferative activity and blocks efficiently the FRS2 phosphorylation in Hep3B cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Hep3B cells
Concentration:

0.3 μM
Incubation Time:

24 h
Result:

Blocked effectively FRS2 phosphorylation.

Cell Proliferation Assay^[1]

Cell Line:

Hep3B cells
Concentration:

0.3 μM
Incubation Time:

24 h
Result:

Had the lowest EC₅₀ value of 5 nM.

Chemical Information

CAS. Nr. 3036751-84-2
Molecular Weight 506.73
Formel C₂₁H₁₄Cl₃N₅O₄
SMILES

ClC(N=C1NC2=NC=C3C(C=CC(C4=C(C(OC)=CC(OC)=C4Cl)Cl)=C3)=N2)=CC=C1[N+]([O-])=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Schwarz M, et al. Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles[J]. Journal of Medicinal Chemistry, 2024. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

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