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Roblitinib (FGF401) FGFR inhibitor

Name: Roblitinib (FGF401)
Brand: Selleck Chemicals
SKU: S8548
Rating: 5 (6 reviews)

Cat.No.S8548

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 a panel of 65 kinases in biochemical assays.

Chemical Structure

Molecular Weight: 506.56

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Quality Control

Batch: Purity: 99.52%

99.52

Related Targets	EGFR VEGFR PDGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other FGFR Inhibitors	PD173074 AZD4547 (Fexagratinib) BLU9931 Futibatinib (TAS-120) LY2874455 PD-166866 Zoligratinib (Debio-1347) H3B-6527 Fisogatinib (BLU-554) SSR128129E

Chemical Information, Storage & Stability

Molecular Weight	506.56	Formula	C₂₅H₃₀N₈O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1708971-55-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CN1CCN(C(=O)C1)CC2=C(N=C3C(=C2)CCCN3C(=O)NC4=NC=C(C(=C4)NCCOC)C#N)C=O

Solubility

In vitro
Batch:

DMSO : 6 mg/mL (11.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.99mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.99mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	FGFR4 (Cell-free assay) 1.9 nM
In vitro	Roblitinib (FGF401) binds in a reversible covalent manner to the FGFR4 kinase domain and inhibits it with an IC50 of 1.9 nM. In biochemical assays, this compound shows at least 1,000 fold selectivity against a panel of 65 kinases, and in a kinome wide scan consisting of 456 kinases, FGFR4 was its only target. It also inhibits growth of HCC and gastric cancer cell lines expressing FG19, FGFR4 and βklotho.
In vivo	In xenograft animal models in vivo, Roblitinib (FGF401) showed a consistent pharmacokinetic/pharmacodynamic (PK/PD) relationship with phospho-FGFR4 over total FGFR4 (p/tFGFR4) levels in tumour robustly inhibited in a dose dependent manner. It has good oral PK properties and remarkable anti-tumour activity in mice bearing HCC tumour xenografts and PDX models that are positive for FGF19, FGFR4 and KLB.
References	[1] http://cancerres.aacrjournals.org/content/77/13_Supplement/2098 [2] https://pubmed.ncbi.nlm.nih.gov/26615127/ [3] http://cancerres.aacrjournals.org/content/77/13_Supplement/2103 [4] https://patents.google.com/patent/WO2015059668A1

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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