Roblitinib (FGF401)

Catalog No.S8548

Roblitinib (FGF401) Chemical Structure

Molecular Weight(MW): 506.56

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.

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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

Solubility (25°C)

In vitro DMSO 5 mg/mL (9.87 mM)
Ethanol 2 mg/mL (3.94 mM)
Water 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 506.56
Formula

C25H30N8O4

CAS No. 1708971-55-4
Storage powder
in solvent
Synonyms N/A

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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