Roblitinib (FGF401)

Catalog No.S8548

For research use only.

Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.1 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays.

Roblitinib (FGF401) Chemical Structure

CAS No. 1708971-55-4

Purity & Quality Control

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Biological Activity

Description Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.1 nM. It binds in a reversible covalent manner to the FGFR4 kinase domain and shows at least 1,000 fold selectivity against of panel of 65 kinases in biochemical assays.
Targets
FGFR4 [1]
(Cell-free assay)
1.1 nM
In vitro

Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and it inhibits FGFR4 with an IC50 of 1.1 nM. In biochemical assays, it shows at least 1,000 fold selectivity against of panel of 65 kinases and in a kinome wide scan, consisting of 456 kinases, FGFR4 was the only target of NVP-FGF401[1]. FGF401 inhibits growth of HCC and gastric cancer cell lines expressing FG19, FGFR4 and βklotho[2].

In vivo In xenograft animal models in vivo, NVP-FGF401 showed a consistent pharmacokinetic/pharmacodynamic (PK/PD) relationship with phospho-FGFR4 over total FGFR4 (p/tFGFR4) levels in tumor robustly inhibited in a dose dependent manner[1]. It has good oral PK properties and remarkable anti-tumor activity in mice bearing HCC tumor xenografts and PDX models that are positive for FGF19, FGFR4 and KLB[3].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 506.56
Formula

C25H30N8O4

CAS No. 1708971-55-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCN(C(=O)C1)CC2=C(N=C3C(=C2)CCCN3C(=O)NC4=NC=C(C(=C4)NCCOC)C#N)C=O

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02325739 Completed Drug: FGF401|Biological: PDR001 Hepatocellular Carcinoma (HCC)|Solid Malignancies Novartis Pharmaceuticals|Novartis December 29 2014 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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