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%
• 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 < .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 o the CDK4/6 inhibitor palbociclib in combination with H3B-6527 could effectively trigger tumor regression in a xenograft model of HC. 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 wit the induction of apoptosis and affects PI3K/Akt and MAPK/ERK pathway.
• 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 determin the effect of blocking FGFR4 in proliferation, invasion, migration, and apoptosis of ESCC cell.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• 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