Roblitinib (Synonyms: FGF-401)

Name: Roblitinib
Brand: MedChemExpress
SKU: HY-101568
Rating: 5.0 (5 reviews)

Cat. No.: HY-101568 Purity: 99.74%: FAQs
Data Sheet SDS COA Handling Instructions

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Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC₅₀ of 1.9 nM. Roblitinib has antitumor activity.

For research use only. We do not sell to patients.

Roblitinib Chemical Structure

CAS No. : 1708971-55-4

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Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE Roblitinib

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

Biological Activity
Purity & Documentation
References
Customer Review

Description

Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC₅₀ of 1.9 nM^[1]. Roblitinib has antitumor activity^[2].

IC₅₀ & Target^[1]^[2]

FGFR4

1.9 nM (IC₅₀)

FGFR1

>10 μM (IC₅₀)

FGFR2

>10 μM (IC₅₀)

FGFR3

>10 μM (IC₅₀)

rat FGFR4

>10 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	24 nM Compound: 6; FGF401	Antiproliferative activity against mouse BaF3 cells transfected with FGFR4 V550M mutant assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against mouse BaF3 cells transfected with FGFR4 V550M mutant assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 36278929]
BaF3	IC₅₀	3 nM Compound: 6; FGF401	Antiproliferative activity against mouse BaF3 cells transfected with human FGFR4 assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against mouse BaF3 cells transfected with human FGFR4 assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 36278929]
BaF3	IC₅₀	5 nM Compound: 6; FGF401	Antiproliferative activity against mouse BaF3 cells transfected with FGFR4 V550L mutant assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against mouse BaF3 cells transfected with FGFR4 V550L mutant assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 36278929]
Hep 3B2	IC₅₀	0.01 μM Compound: 6; FGF401	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 5 days by SRB analysis Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 5 days by SRB analysis	[PMID: 36278929]
Hep 3B2	IC₅₀	8.8 nM Compound: FGF401	Antiproliferative activity against human Hep3B cells with high FGFR4 expression assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo method Antiproliferative activity against human Hep3B cells with high FGFR4 expression assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo method	[PMID: 30987781]
Huh-7	IC₅₀	0.026 μM Compound: 6; FGF401	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 5 days by SRB analysis Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 5 days by SRB analysis	[PMID: 36278929]
Huh-7	IC₅₀	16.3 nM Compound: FGF401	Antiproliferative activity against human HuH7 cells with high FGFR4 expression assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo method Antiproliferative activity against human HuH7 cells with high FGFR4 expression assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo method	[PMID: 30987781]
NCI-H1299	IC₅₀	16.2 μM Compound: 6; FGF401	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 5 days by SRB analysis Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth measured after 5 days by SRB analysis	[PMID: 36278929]

In Vitro

Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (IC₅₀= 1.9 nM)^[1].
Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC₅₀>10 uM)^[1].
Roblitinib inhibits HUH7 (IC₅₀=12 nM), Hep3B (IC₅₀=9 nM), JHH7 (IC₅₀=9 nM), HEPG2 (IC₅₀>10 uM), JHH (IC₅₀>10 uM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model^[1].
Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days^[1].
Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T_1/2 of 1.4 hours, a CL of 28 mL/min?kg, and a V_ss of 2.3 L/kg for Male mice (C57BL/6) ^[1].
Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T_1/2 of 4.4 hours, a CL of 19 mL/min?kg, and a V_ss of 3.9 L/kg for male SD rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar Hannover rats (Hep3B xenograft model)^[1]
Dosage:	10, 30, 100 mg/kg
Administration:	Gavage; for 10 days
Result:	Caused blood concentrations dropped below the IC90 threshold between 8 and 12 h following dosing. Had the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model.

Animal Model:	Male mice (C57BL/6)^[1]
Dosage:	1 mg/kg or 3 mg/kg (Pharmacokinetic Analysis)
Administration:	IV at 1 mg/kg; PO at 3 mg/kg
Result:	Had a T_1/2 of 1.4 hours, a CL of 28 mL/min•kg, and a V_ss of 2.3 L/kg.

Clinical Trial

Molecular Weight

506.56

Formula

C₂₅H₃₀N₈O₄

CAS No.

1708971-55-4

Appearance

Solid

Color

White to off-white

SMILES

CN1CC(N(CC2=CC(CCCN3C(NC4=CC(NCCOC)=C(C#N)C=N4)=O)=C3N=C2C=O)CC1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (9.87 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9741 mL	9.8705 mL	19.7410 mL
5 mM	0.3948 mL	1.9741 mL	3.9482 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.74%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (251 KB) HNMR (255 KB) RP-HPLC (223 KB)

Handling Instructions (2659 KB)

References

[1]. Nicole Buschmann, et al. Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors. WO2015059668A1.

[2]. Robin A Fairhurst, et al. Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4. J Med Chem. 2020 Nov 12;63(21):12542-12573. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9741 mL	9.8705 mL	19.7410 mL	49.3525 mL
DMSO	5 mM	0.3948 mL	1.9741 mL	3.9482 mL	9.8705 mL

Roblitinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Roblitinib1708971-55-4FGF-401FGF401FGF 401FGFRFibroblast growth factor receptorC552AHUH7Hep3BJHH7HEPG2JHHInhibitorinhibitorinhibit

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Roblitinib (Synonyms: FGF-401)

Customer Review

Roblitinib Related Antibodies

5 Publications Citing Use of MCE Roblitinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All FGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Roblitinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Roblitinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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