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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.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| 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. |
| Formula | C21H14Cl3N5O4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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