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Art. -Nr.: HY-163569

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FGFR4-IN-20

FGFR4-IN-20 (comp 11) is an orally active and selective FGFR4 inhibitor with IC₅₀s of 19 and 36 nM against Huh7 cells and FGFR4 enzyme. FGFR4-IN-20 can be used for hepatocellular carcinoma research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₆H₂₂Cl₂N₄O₃
Molecular Weight:509.38

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

FGFR4-IN-20 Chemical Structure

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

FGFR4

Cellular Effect

Cell Line	Type	Value	Description	References
Hep 3B2	GI₅₀	16 nM Compound: 11	Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Hep3B cells by SRB assay Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Hep3B cells by SRB assay	[PMID: 38706130]
Hep 3B2	IC₅₀	16 nM Compound: 11	Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay Antiproliferative activity against FGF19 amplified human Hep3B cells assessed as inhibition of cell growth by SRB assay	[PMID: 38706130]
HepG2	GI₅₀	335 nM Compound: 11	Growth inhibition of human HepG2 cells by SRB assay Growth inhibition of human HepG2 cells by SRB assay	[PMID: 38706130]
HS27	GI₅₀	913 nM Compound: 11	Growth inhibition of human HS27 cells by SRB assay Growth inhibition of human HS27 cells by SRB assay	[PMID: 38706130]
Huh-7	GI₅₀	16 nM Compound: 11	Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Huh-7 cells by SRB assay Growth inhibition of FGF19 amplified and FGFR4 overexpressing human Huh-7 cells by SRB assay	[PMID: 38706130]
Huh-7	IC₅₀	19 nM Compound: 11	Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay Antiproliferative activity against FGFR4 overexpressing human Huh-7 cells assessed as inhibition of cell growth by SRB assay	[PMID: 38706130]
PLC-PRF-5	GI₅₀	598 nM Compound: 11	Growth inhibition of human PLCPRF5 cells by SRB assay Growth inhibition of human PLCPRF5 cells by SRB assay	[PMID: 38706130]
RT-112	GI₅₀	151 nM Compound: 11	Growth inhibition of FGFR3 overexpressing human RT-112 cells by SRB assay Growth inhibition of FGFR3 overexpressing human RT-112 cells by SRB assay	[PMID: 38706130]
SNU-387	GI₅₀	251 nM Compound: 11	Growth inhibition of human SNU-387 cells by SRB assay Growth inhibition of human SNU-387 cells by SRB assay	[PMID: 38706130]

In Vitro

FGFR4-IN-20 (0.01-1000 nM) shows IC₅₀s of 19, 16 and 33 nM against Huh7 (FGFR4 overexpression), Hep3B (FGF19 amplification) and JHH-7 (FGF19 amplification) cell lines, respectively^[1].

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

In Vivo

FGFR4-IN-20 (100mg/kg, p.o., QD for 15 d) significantly reduces the tumor volumes of ICR mice without a loss of body weight or other clinical signs^[1].
1.19
Pharmacokinetics Profile of FGFR4-IN-20 in ICR Mice^[1]

Parameter	IV (5 mg/kg)	PO (100 mg/kg, QD)
AUC_0-24 (ng·h/mL)	4810	59534
C_max (ng/mL)	8137	24566
T_max (h)		0.5
T_1/2 (h)	1.7	3.9
F%		61.9

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

Chemical Information

Molecular Weight 509.38
Formel C₂₆H₂₂Cl₂N₄O₃
SMILES

ClC1=C(C2=CC3=CN=C(C=C3C(C)=N2)NC4=C(C=CC=C4)NC(C=C)=O)C(Cl)=C(OC)C=C1OC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)
Handling Instructions (2659 KB)

Verweise

[1]. Oh H, et al. Discovery of 2,6-Naphthyridine Analogues as Selective FGFR4 Inhibitors for Hepatocellular Carcinoma. J Med Chem. 2024 May 23;67(10):8445-8459. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

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