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Art. -Nr.: HY-189204

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FGFR2-IN-4

FGFR2-IN-4 is a selective, orally active FGFR2 inhibitor, with IC₅₀ values of 10.0 nM and 5.8 nM against wild-type FGFR2 and the FGFR2^V565F mutant, respectively. FGFR2-IN-4 induces necroptosis in FGFR2-driven tumor cells. FGFR2-IN-4 induces tumor regression in xenograft models harboring FGFR2 inhibitor-resistant mutations without altering serum phosphate levels. FGFR2-IN-4 is used to investigate FGFR2-driven malignancies, including intrahepatic cholangiocarcinoma and gastric cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3110002-64-4
Formel: C₂₅H₂₀N₈O
Molecular Weight:448.48

Speicherung:

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

FGFR2-IN-4 Chemical Structure

CAS. Nr.: 3110002-64-4

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Use of MCE Products

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

^[1]

FGFR2

10.0 nM (IC₅₀)

FGFR2^V565F

5.8 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
KATO III stomach cancer cell line	IC50	9.0 nM	Antiproliferative effect against FGFR2-amplified KATOIII human gastric cancer cells. Antiproliferative effect against FGFR2-amplified KATOIII human gastric cancer cells.	42675086
BaF3	IC50	37.6 nM	Antiproliferative activity against FGFR2 N550K mutant-expressing Ba/F3 cells incubated for 3 days assessed by CellTiter-Glo luminescence assay. Antiproliferative activity against FGFR2 N550K mutant-expressing Ba/F3 cells incubated for 3 days assessed by CellTiter-Glo luminescence assay.	42675086

In Vitro

FGFR2-IN-4 (Compound LC-F2-1) (1 nM-1000 nM) potently inhibits both FGFR2 wild-type (IC₅₀ = 10.0 nM) and the FGFR2 V565F resistance mutant (IC₅₀ = 5.8 nM) with high selectivity over FGFR1, FGFR4, and the majority of the 416 screened human kinases^[1].
FGFR2-IN-4 (3 days) displays strong cellular isoform selectivity for FGFR2 over FGFR1, FGFR3, and FGFR4 in engineered Ba/F3 proliferation assays, with an IC₅₀ of 4.0 nM against FGFR2-driven cell growth^[1].
FGFR2-IN-4 engages FGFR2 in KATOIII cells via stable, irreversible covalent binding, as demonstrated by persistent suppression of FGFR2 downstream signaling even after the unbound compound is completely washed out^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

Ba/F3 cells expressing FGFR1, FGFR2, FGFR3, or FGFR4
Concentration:

9-point threefold serial dilutions
Incubation Time:

3 days
Result:

Inhibits the proliferation of FGFR2-expressing Ba/F3 cells with an IC₅₀ of 4.0 nM.
Results in 44-fold reduced sensitivity in FGFR1-expressing cell line with an IC₅₀ of 175.9 nM.
Results in 23-fold reduced sensitivity in FGFR3-expressing cell line with an IC₅₀ of 93.4 nM.
Shows no detectable anti-proliferative activity in FGFR4-expressing Ba/F3 cells.

In Vivo

FGFR2-IN-4 (10 mg/kg; p.o., once daily for 14 consecutive days) achieves 87% tumor growth inhibition in mouse xenograft models bearing FGFR2^V565F without inducing elevated serum phosphate levels^[1].
FGFR2-IN-4 (10 mg/kg; p.o.; once daily for 11 consecutive days) exhibits potent antitumor activity in the FGFR2^M538I xenograft mouse model^[1].

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

Animal Model:

BALB/c mice (female, 6 weeks old)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 14 days
Result:

Produced 87% tumor growth inhibition.
Maintained stable body weight throughout the 14-day period.
Kept serum phosphate levels within the normal physiological range.

Animal Model:

BALB/c mice (female, 6 weeks old)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 11 days
Result:

Exerted pronounced antitumor activity against FGFR2 M538I mutant tumors.
Achieved significant reduction in tumor weight relative to vehicle-treated animals.

Chemical Information

CAS. Nr. 3110002-64-4
Molecular Weight 448.48
Formel C₂₅H₂₀N₈O
SMILES

C=CC(NC1=CC=C(C2=C(C#CC3=CN=C(N(C)C=N4)C4=C3)C5=C(N)N=CN=C5N2C)C=C1)=O
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]. Huang X, et al. Discovery of a covalent FGFR2-selective inhibitor overcoming clinically-acquired resistance mutations. Nature communications. 2026 Aug 03;17(1):9326.

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

Keywords

MOQ

Minimum order quantity

100 mg

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