FGFR3-IN-11
FGFR3-IN-11(compound B11) is a Fibroblast growth factor receptor 3 (FGFR3) inhibitor with a Ka value of 4.8 μM. FGFR3-IN-11 induces apoptosis, suppresses colony formation, and causes dose-dependent G0/G1 cell cycle arrest in cancer cells. FGFR3-IN-11 exerts anticancer activity against cancer cells with minimal toxicity toward normal hepatocytes and demonstrates tumor growth suppression in xenograft mouse models. FGFR3-IN-11 can be used for the research of hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Formula: C27H35N3OS
- Molecular Weight:449.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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FGFR3 |
FGFR3-IN-11 (B10) (48 h) potently inhibits the proliferation of Huh-7, HepG2, and MHCC97-H hepatocellular carcinoma cell lines with IC50 values of 4.13, 4.76, and 5.79 μM, respectively, and has minimal toxicity to L02 normal hepatocytes[1].
FGFR3-IN-11 (B10) (1.25-5 μM; 48 h initial treatment, 14 days medium replacement) suppresses colony formation in Huh-7 hepatocellular carcinoma cells in a dose-dependent manner[1].
FGFR3-IN-11 (B10) (1.25-5 μM; 48 h) induces dose-dependent G0/G1 phase arrest in Huh-7 hepatocellular carcinoma cells[1].
FGFR3-IN-11 (B10) (1.25-5 μM; 24 h) induces dose-dependent apoptosis in Huh-7 hepatocellular carcinoma cells, with corresponding changes in Bcl-2 and Bax protein levels[1].
FGFR3-IN-11 (B10) (1.25-5 μM; 24 h) inhibits the PI3K/AKT signaling pathway in Huh-7 hepatocellular carcinoma cells by dose-dependently reducing total and phosphorylated PI3K and AKT levels[1].
FGFR3-IN-11 (B10) (serial dilutions, 40 μM, 10-40 μM; 1 h DARTS pre-incubation) stably binds to FGFR3 protein with a KD of 4.8 μM, as validated by molecular docking, SPR, CETSA, and DARTS assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh-7
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Concentration:1.25-5 μM
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Incubation Time:48 h (initial treatment); 14 days (medium replacement)
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Result:Significantly suppressed colony formation in Huh-7 cells in a dose-dependent manner.
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Cell Line:Huh-7
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Concentration:1.25-5 μM
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Incubation Time:48 h
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Result:Induced dose-dependent G0/G1 phase arrest in Huh-7 cells.
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Cell Line:Huh-7
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Concentration:1.25-5 μM
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Incubation Time:24 h
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Result:Induced dose-dependent apoptosis in Huh-7 cells. Downregulated anti-apoptotic protein Bcl-2 and upregulated pro-apoptotic protein Bax in a dose-dependent manner (Western blot).
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Cell Line:Huh-7
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Concentration:1.25-5 μM
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Incubation Time:24 h
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Result:Reduced the levels of total and phosphorylated PI3K and AKT in a dose-dependent manner.
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 mice (female, 4-6 weeks old, 18-19 g average weight)[1]
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Dosage:20, 40, 60 mg/kg; 40 mg/kg (TGI assessment)
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Administration:i.p.; every other day; 28 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 64.18% at 40 mg/kg; Induced a dose-dependent decrease in phospho-FGFR3 (p-FGFR3) in tumor tissues; Caused a pronounced decrease in Ki-67-positive cells in tumors; Showed no significant weight loss compared to the control group.
Chemical Information
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Molecular Weight 449.65
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Formula C27H35N3OS
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SMILES
O=C(C1=CC2=C(N3C[C@@]4(CCCN5CCC[C@@]([C@@]54[H])([C@]3(CC2)[H])[H])[H])S1)NC6=CC=C(C(C)C)C=C6
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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)
FGFR3-IN-11 Related Classifications
HY-181152 Related Classifications
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