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Art. -Nr.: HY-183780

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FGFR-IN-27

FGFR-IN-27 is an orally active, broad-spectrum FGFR inhibitor, with an IC₅₀ of 0.24 nM against human FGFR1, 0.71 nM against FGFR2, 0.87 nM against FGFR3, and 6.50 nM against FGFR4. FGFR-IN-27 inhibits cancer cell proliferation and blocks tumor growth. FGFR-IN-27 reduces the phosphorylation levels of AKT and ERK, induces apoptosis and ferroptosis, increases ROS levels, and decreases GSH levels. FGFR-IN-27 can be used in the research of hepatocellular carcinoma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₈H₃₂Cl₂N₆O₃
Molecular Weight:571.50

Speicherung:

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

FGFR-IN-27 Chemical Structure

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

FGFR1

0.24 nM (IC₅₀)

FGFR2

0.71 nM (IC₅₀)

FGFR3

0.87 nM (IC₅₀)

FGFR4

6.5 nM (IC₅₀)

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In Vitro

FGFR-IN-27 (Compound 1a) (0.1 nM-10000 nM; 3 days) inhibits the proliferation of human Huh7, MHCC97-H, HepG2, MCF7 and MDA-MB-231 cells, with IC₅₀ values of 11.0 nM, 91.2 nM, 485 nM, 4430 nM and 3380 nM, respectively^[1].
FGFR-IN-2 inhibits migration and proliferation of human Huh7 hepatocellular carcinoma cells^[1].
FGFR-IN-27 (0.01-10 μM) inhibits the downstream signaling pathway of FGFR in human Huh7 hepatocellular carcinoma cells by dose-dependently reducing the phosphorylation levels of AKT and ERK^[1].
FGFR-IN-27 (10-100 nM; 24 h) induces apoptosis in human Huh7 hepatocellular carcinoma cells^[1].
FGFR-IN-27 (0.1 μM) induces ferroptosis in human Huh7 hepatocellular carcinoma cells, increases ROS levels, and decreases glutathione (GSH) levels^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

human hepatocellular carcinoma Huh7, MHCC97-H, HepG2 cells; human breast cancer MCF7, MDA-MB-231 cells
Concentration:

0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time:

3 days
Result:

Inhibited proliferation of Huh7 cells with an IC₅₀ of 11.0 nM.
Inhibited proliferation of MHCC97-H cells with an IC₅₀ of 91.2 nM.
Inhibited proliferation of HepG2 cells with an IC₅₀ of 485 nM.
Inhibited proliferation of MCF7 cells with an IC₅₀ of 4430 nM.
Inhibited proliferation of MDA-MB-231 cells with an IC₅₀ of 3380 nM.

Apoptosis Analysis^[1]

Cell Line:

human hepatocellular carcinoma Huh7 cells
Concentration:

10, 50, 100 nM
Incubation Time:

24 h
Result:

Induced apoptosis in Huh7 cells significantly at 10 nM.
Induced apoptosis in Huh7 cells significantly at 50 nM.
Induced apoptosis in Huh7 cells significantly at 100 nM.
Increased apoptosis rates of Huh7 cells with higher concentrations.

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	AUC_0-24	MRT	Bioavailability	T_max
Mice^[1]	2 mg/kg	i.v.	1.20 h	8540 ng/mL	2501 ng·h/mL	0.63 h	66.9 %	/
Mice^[1]	5 mg/kg	p.o.	0.995 h	4694 ng/mL	4156 ng·h/mL	1.08 h	66.9 %	0.25 h

In Vivo

FGFR-IN-27 (10-50 mg/kg; p.o.; once daily; for 15 consecutive days) achieves tumor growth inhibition rates of 54.5% and 90.5%, respectively, in BALB/c nude mice bearing Huh7 hepatocellular carcinoma xenografts, with no systemic toxicity observed^[1].

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

Animal Model:

BALB/c nude (female, 8 weeks old)^[1]
Dosage:

10 mg/kg; 50 mg/kg
Administration:

p.o.; daily; 15 days
Result:

Achieved a 54.5% tumor growth inhibition (TGI) rate.
Achieved a 90.5% TGI rate, nearly completely suppressing tumor growth.
Caused no significant mouse weight loss throughout the study.
Showed no significant toxicity in major organs (lung, liver, spleen, kidney, heart) via hematoxylin and eosin (HE) staining at therapeutic doses.

Related Protocols :

Chemical Information

Molecular Weight 571.50
Formel C₂₈H₃₂Cl₂N₆O₃
SMILES

CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC4=C(CN(C(N4C)=O)C5=C(C(OC)=CC(OC)=C5Cl)Cl)C=N3
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

Handling Instructions (2659 KB)

Verweise

[1]. Yang Y, et al. Design of fibroblast growth factor receptor (FGFR) inhibitors containing a 3,4-dihydropyrido[4,3-d]pyrimidin-2(1H)-one motif. Eur J Med Chem. 2026 Sep 15;314:118912. [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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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FGFR-IN-27

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