For research use only.

Catalog No.S8675

3 publications

H3B-6527 Chemical Structure

CAS No. 1702259-66-2

H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively).

Selleck's H3B-6527 has been cited by 3 publications

1 Customer Review

  • KYSE150 and KYSE450 cells were treated each day with 1 μM H3B‐6527 or left untreated for three days, and lysates were immunoblotted with indicated antibodies. Western blotting demonstrated that the expression of EMT‐related markers (E‐cadherin, N‐cadherin, Claudin‐1, Vimentin, and Snail) was altered with FGFR4 blockade.

    Thorac Cancer, 2018, 9(12):1687-1698. H3B-6527 purchased from Selleck.

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Biological Activity

Description H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively).
FGFR4 [1]
(Cell-free assay)
<1.2 nM
In vitro

H3B-6527 shows robust inhibition of the target kinase FGFR4 with an IC50 value of <1.2 nmol/L and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nmol/L respectively). TAOK2, JNK2, and CSF1R are also less sensitive to H3B-6527 treatment with IC50 values of 690, >10,000, and >10,000 nmol/L, respectively. H3B-6527 inhibits FGFR4 signaling, proliferation, and leads to apoptosis in a HCC cell line (Hepatocellular carcinoma). Treatment on Hep3B cells leads to robust activation of caspase-3/7, an apoptotic marker, in a concentration-dependent manner, indicating FGFR4 inhibition by H3B-6527 leads to cell death in HCC cell lines. H3B-6527 has the selectivity and the selective dependence on FGFR4 across cancer types[1].

In vivo In the Hep3B human HCC xenograft mouse model, H3B-6527 shows dose-proportional plasma exposures and greater than dose-proportional tumor exposures within the dose range evaluated (30, 100, and 300 mg/kg). The H3B-6527 pharmacodynamic response as measured by CYP7A1 mRNA and pERK1/2 protein levels is dose dependent, with higher doses leading to sustained responses. Oral treatment of H3B-6527, twice daily, inhibits xenograft growth in a dose-dependent manner in nude mice, with the 300 or 100 mg/kg twice daily, significantly inhibiting tumor growth in both Hep3B subcutaneous and orthotopic xenograft model and causing tumor regressions in the subcutaneous xenograft model. Palbociclib can enhance H3B-6527 efficacy and promote tumor regression in JHH-7 model where H3B-6527 as a single agent can only lead to tumor stasis[1].


Cell Research:


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  • Cell lines: Hep3B cells
  • Concentrations: 100 and 300 nmol/L
  • Incubation Time: 0.5, 1, 2, 4, 8, and 24 hours
  • Method:

    Hep3B cells are treated with H3B-6527 at 100 and 300 nmol/L for 0.5, 1, 2, 4, 8, and 24 hours and pERK1/2 levels are measured.

    (Only for Reference)
Animal Research:


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  • Animal Models: BALB/c nu/nu female mice
  • Dosages: 30, 100, and 300 mg/kg
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 50 mg/mL (79.42 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 629.54


CAS No. 1702259-66-2
Storage powder
in solvent
Synonyms N/A
Smiles CCN1CCN(CC1)C2=CC(=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl)NC(=O)C=C

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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03424577 Completed Drug: H3B-6527 Healthy Participants Eisai Inc.|H3 Biomedicine Inc. December 27 2017 Phase 1
NCT02834780 Active not recruiting Drug: H3B-6527 Advanced Hepatocellular Carcinoma|Hepatocellular Carcinoma|Liver Cancer|Liver Neoplasms|Hepatic Cancer|Hepatic Carcinoma H3 Biomedicine Inc.|Eisai Inc. July 2016 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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FGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID