Cat. No.: HY-101568

Roblitinib

(Synonyms: FGF-401)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

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

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Pureté: 99.67%
CAS No.: 1708971-55-4
Formule: C₂₅H₃₀N₈O₄
Masse moléculaire:506.56

Stockage:

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

Roblitinib Chemical Structure

CAS No.: 1708971-55-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

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	>2000 nM Compound: 3; FGF401	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell growth	[PMID: 38348819]
BaF3	IC₅₀	1.7 nM Compound: 3; FGF401	Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550L mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
BaF3	IC₅₀	21.6 nM Compound: 3; FGF401	Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring FGFR4 V550M mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
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	4 nM Compound: 3; FGF401	Antiproliferative activity against mouse BaF3 cells harboring wild type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring wild type FGFR4 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
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]
HEK293	IC₅₀	>2000 nM Compound: 3; FGF401	Cytotoxicity against HEK293 cells assessed as inhibition of cell growth Cytotoxicity against HEK293 cells assessed as inhibition of cell growth	[PMID: 38348819]
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	0.01 μM Compound: 3; FGF401	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
Hep 3B2	IC₅₀	210 nM Compound: 8	Cytotoxicity against human Hep 3B2.1-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth Cytotoxicity against human Hep 3B2.1-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth	[PMID: 35119278]
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]
Huh-7	IC₅₀	19.7 nM Compound: 3; FGF401	Antiproliferative activity against FGF19/FGFR4 dependent human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against FGF19/FGFR4 dependent human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 38348819]
Huh-7	IC₅₀	8.9 nM Compound: 8	Cytotoxicity against human Huh-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth Cytotoxicity against human Huh-7 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth	[PMID: 35119278]
MDA-MB-453	IC₅₀	920 nM Compound: 8	Cytotoxicity against human MDA-MB-453 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth Cytotoxicity against human MDA-MB-453 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth	[PMID: 35119278]
NCI-H1299	IC₅₀	15.3 μM Compound: 3; FGF401	Antiproliferative activity against FGFR4 independent human NCI-H1299 cells assessed as inhibition of cell growth Antiproliferative activity against FGFR4 independent human NCI-H1299 cells assessed as inhibition of cell growth	[PMID: 38348819]
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]
NCI-H1581	IC₅₀	>3 μM Compound: 8	Cytotoxicity against human NCI-H1581 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth Cytotoxicity against human NCI-H1581 cells harboring FGF19/FGFR4 assessed as inhibition of cell growth	[PMID: 35119278]

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1708971-55-4
Appearance Solid
Masse moléculaire 506.56
Formule C₂₅H₃₀N₈O₄
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
Synonyms

FGF-401
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (9)

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Nat Commun

N6-methyladenosine regulated FGFR4 attenuates ferroptotic cell death in recalcitrant HER2-positive breast cancer. [Abstract]

2022 May 13;13(1):2672. PMID: 35562334
Adv Sci (Weinh)

Lipid-Driven OLR1/FOXM1/FGF19 Axis Orchestrates Crosstalk in an Epithelial-Fibroblast Positive Feedback Promoting Progesterone Resistance in Endometrial Cancer. [Abstract]

2025 Nov 21:e11943. PMID: 41270216
Cell Rep Med

Single-cell profiles delineate immune cell remodeling and enhanced tumor-fibroblast interaction of hepatoblastoma after chemotherapy. [Abstract]

2025 Oct 21;6(10):102401. PMID: 41038160
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Cancer Cell Int

The anti-tumor effects of AZD4547 on ovarian cancer cells: differential responses based on c-Met and FGF19/FGFR4 expression. [Abstract]

2024 Jan 25;24(1):43. PMID: 38273381
Int Immunopharmacol

FGFR4 inhibition augments paclitaxel-induced cell death in ovarian cancer. [Abstract]

2025 Apr 16:155:114626. PMID: 40245772
J Cancer

Highly Potent Immunotoxins Targeting the Membrane-distal N-lobe of GPC3 for Immunotherapy of Hepatocellular Carcinoma. [Abstract]

2022 Feb 14;13(4):1370-1384. PMID: 35281879
University of Auckland

2025.
Biochemistry for Health, NOVA University of Lisbon

2019 Jul.

Solvant et solubilité

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)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9741 mL

9.8705 mL

19.7410 mL

5 mM

0.3948 mL

1.9741 mL

3.9482 mL

10 mM

---

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Roblitinib

9 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Roblitinib

Activité biologique

Chemical Information

Publications (9)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Roblitinib Related Classifications

HY-101568 Related Classifications