H3B-6527

H3B-6527，一种通过结构指导药物设计而成的高度选择性共价FGFR4抑制剂。在40种HCC细胞系和30种HCC PDX模型的研究表明，FGF19表达是预测H3B-6527反应的生物标志物。此外，与CDK4/6抑制剂palbociclib联合使用H3B-6527能有效触发HCC异种移植模型的肿瘤退化[1]。FGFR4在ESCC组织和细胞系中经常过表达。体外实验表明，通过特异性阻断剂H3B-6527阻断FGFR4，显著降低了ESCC细胞的增殖、侵袭和迁移，改变了上皮-间充质转换标记物。此外，FGFR4阻断与诱导凋亡有关，并影响PI3K/Akt和MAPK/ERK途径[2]。

DMSO:6.3 mg/mL (10 mM)

Immunohistochemistry and Western blotting were used to detect FGFR4 expression in ESCC samples and cell lines. Cell counting kit-8, and clonogenic, transwell, flow cytometric, and tumor xenograft in nude mice assays were utilized to determine the effect of blocking FGFR4 in proliferation, invasion, migration, and apoptosis of ESCC cells[2].