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FGFR4-IN-19

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Catalog No. T209757

FGFR4-IN-19 (compound 8B) is a potent covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 value of 1.2 nM. It achieves high efficiency and selectivity by covalently targeting the rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 is applicable for hepatocellular carcinoma (HCC) research.

FGFR4-IN-19

FGFR4-IN-19

🥰Excellent
Catalog No. T209757
FGFR4-IN-19 (compound 8B) is a potent covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 value of 1.2 nM. It achieves high efficiency and selectivity by covalently targeting the rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 is applicable for hepatocellular carcinoma (HCC) research.
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Product Introduction

Bioactivity
Description
FGFR4-IN-19 (compound 8B) is a potent covalent inhibitor of fibroblast growth factor receptor 4 (FGFR4) with an IC50 value of 1.2 nM. It achieves high efficiency and selectivity by covalently targeting the rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 is applicable for hepatocellular carcinoma (HCC) research.
Targets&IC50
FGFR1:4370 nM, FGFR2:490 nM, FGFR3:>5000 nM, FGFR4:1.2 nM
In vitro
FGFR4-IN-19 exhibits weak inhibitory activity against FGFR1 (IC 50 = 4.4 μM) and FGFR2 (IC 50 = 490 nM), with all other IC 50 values exceeding 5 μM. This compound shows high selectivity within the FGFR family. It demonstrates effective cellular FGFR4 binding (EC 50 = 52±7 nM) relative to FGFR1-3 (IC 50 >10 μM). Additionally, FGFR4-IN-19 (0.3 μM, 24 h) shows significant antiproliferative activity, effectively blocking the phosphorylation process of FRS2 in Hep3B cells.
Chemical Properties
FormulaC21H14Cl3N5O4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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