Home Protein Tyrosine Kinase FGFR inhibitor Roblitinib (FGF401) For research use only.

Roblitinib (FGF401)

Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.9 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

Roblitinib (FGF401) Chemical Structure

CAS: 1708971-55-4

Selleck's Roblitinib (FGF401) has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.52%
99.52

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Signaling Pathway

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FGFR Signaling Pathway

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Biological Activity

Description Roblitinib (FGF401) is an FGFR4-selective inhibitor with an IC50 of 1.9 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)
1.9 nM
In vitro
In vitro

Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and it inhibits FGFR4 with an IC50 of 1.9 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 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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02325739 Completed
Hepatocellular Carcinoma (HCC)|Solid Malignancies
Novartis Pharmaceuticals|Novartis
 December 29 2014 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 506.56 Formula

C25H30N8O4
CAS No. 1708971-55-4 SDF --
Smiles CN1CCN(C(=O)C1)CC2=C(N=C3C(=C2)CCCN3C(=O)NC4=NC=C(C(=C4)NCCOC)C#N)C=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 6 mg/mL ( (11.84 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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