化合物H3B-6527 T7738

Product Introduction
Bioactivity


英文名: H3B-6527

描述: H3B-6527 是一种在 FGF19 驱动的肝细胞癌中有效且选择性的 FGFR4 抑制剂，具有抗肿瘤活性。

细胞实验: 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].

体外活性: H3B-6527, a highly selective covalent FGFR4 inhibitor, through structure-guided drug design. Studies in a panel of 40 HCC cell lines and 30 HCC PDX models showed that FGF19 expression is a predictive biomarker for H3B-6527 response. Moreover, coadministration of the CDK4/6 inhibitor palbociclib in combination with H3B-6527 could effectively trigger tumor regression in a xenograft model of HCC[1].?FGFR4 is frequently overexpressed in ESCC tissue and cell lines. in vitro assays have shown that blocking FGFR4 by a specific blocker, H3B-6527, significantly decreases proliferation, invasion, and migration, and alters epithelial-mesenchymal transition markers in ESCC cells. In addition, FGFR4 blockade is associated with the induction of apoptosis and affects PI3K/Akt and MAPK/ERK pathways[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 6.3 mg/mL (10 mM)


关键字: H3B6527 | H-3B-6527 | H3B 6527 | H3B-6527

相关产品: TAK-632 | Sucralfate | Mubritinib | Orantinib | FIIN-2 | KW-2449 | SUN11602 | Infigratinib | Ferulic Acid | Heparan Sulfate

相关库: Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Highly Selective Inhibitor Library | Tyrosine Kinase Inhibitor Library | Apoptosis Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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