H3B-6527

SKU: orb1299550

Description

H3B-6527 is a potent, selective FGFR4 inhibitor developed for FGF19-driven hepatocellular carcinoma research. It demonstrates antineoplastic activity in both in vitro cell-based assays and in vivo xenograft models, making it a key tool for studying targeted HCC therapies.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1702259-66-2
• MW: 629.54
• Purity: 99.85% (May vary between batches)
• Formula: C₂₉H₃₄Cl₂N₈O₄
• SMILES: CCN1CCN(CC1)c1ccc(Nc2cc(ncn2)N(C)C(=O)Nc2c(Cl)c(OC)cc(OC)c2Cl)c(NC(=O)C=C)c1
• Target: FGFR
• Solubility: DMSO:6.3 mg/mL (10.01 mM)

Bioactivity

• Target IC50:
  FGFR2:1290 nM|FGFR1:320 nM|FGFR3:1060 nM|FGFR4:<1.2 nM
• In Vitro:
  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. 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.
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• Cell Research:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

H3B 6527, H3B6527, H-3B-6527, H3B-6527, FGFR

Compound Identifiers

PubChem CID

118029202