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.
For research use only. We do not sell to patients.
- Formula: C28H32Cl2N6O3
- Molecular Weight:571.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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FGFR1 0.24 nM (IC50) |
FGFR2 0.71 nM (IC50) |
FGFR3 0.87 nM (IC50) |
FGFR4 6.5 nM (IC50) |
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.
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Cell Line:human hepatocellular carcinoma Huh7, MHCC97-H, HepG2 cells; human breast cancer MCF7, MDA-MB-231 cells
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Concentration:0.1, 1, 10, 100, 1000, 10000 nM
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Incubation Time:3 days
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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.
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Cell Line:human hepatocellular carcinoma Huh7 cells
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Concentration:10, 50, 100 nM
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Incubation Time:24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 8 weeks old)[1]
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Dosage:10 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 15 days
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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.
Chemical Information
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Molecular Weight 571.50
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Formula C28H32Cl2N6O3
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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