2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. 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.

For research use only. We do not sell to patients.

FGFR4-IN-19 Chemical Structure

FGFR4-IN-19 Chemical Structure

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FGFR4-IN-19 Related Antibodies

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Description

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[1].

IC50 & Target[1]

FGFR4

1.2 nM (IC50)

FGFR1

4370 nM (IC50)

FGFR2

490 nM (IC50)

FGFR3

>5000 nM (IC50)

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.

FGFR4-IN-19 Related Antibodies

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.
Molecular Weight

506.73

Formula

C21H14Cl3N5O4
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FGFR4-IN-19 Related Classifications

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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:

FGFR4-IN-19FGFRFibroblast growth factor receptorFGFR4 inhibitorHep3B cellshepatocellular carcinomaFRS2 phosphorylationInhibitorinhibitorinhibit

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FGFR4-IN-19
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HY-158248
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