| Bioactivity | 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]. |
| Invitro | FGFR4-IN-19 对 FGFR1 (IC50=4.4 μM) 和 FGFR2 (IC50=490 nM) 的抑制活性较弱，其余 IC50 值均在 5 μM 以上。 FGFR4-IN-19 在 FGFR 家族中具有高度选择性[1]。FGFR4-IN-19 显示出有效的细胞 FGFR4 结合性 (EC50= 52±7 nM) 相比于 FGFR1-3 (IC50>10 μM)[1]。FGFR4-IN-19 (0.3 μM， 24 h) 表现出良好的抗增殖活性，可有效阻断 Hep3B 细胞中的 FRS2 磷酸化进程[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> FGFR4-IN-19 相关抗体: Western Blot Analysis[1] Cell Line: |
| Formula | C21H14Cl3N5O4 |
| Molar Mass | 506.73 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Schwarz M, et al. Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles[J]. Journal of Medicinal Chemistry, 2024. |