2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. 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.

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FGFR3-IN-11

FGFR3-IN-11 Chemical Structure

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FGFR3-IN-11 Related Antibodies

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Description

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[1].

IC50 & Target[1]

FGFR3

 

In Vitro

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.

FGFR3-IN-11 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Huh-7
Concentration: 1.25-5 μM
Incubation Time: 48 h (initial treatment); 14 days (medium replacement)
Result: Significantly suppressed colony formation in Huh-7 cells in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: Huh-7
Concentration: 1.25-5 μM
Incubation Time: 48 h
Result: Induced dose-dependent G0/G1 phase arrest in Huh-7 cells.

Apoptosis Analysis[1]

Cell Line: Huh-7
Concentration: 1.25-5 μM
Incubation Time: 24 h
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).

Western Blot Analysis[1]

Cell Line: Huh-7
Concentration: 1.25-5 μM
Incubation Time: 24 h
Result: Reduced the levels of total and phosphorylated PI3K and AKT in a dose-dependent manner.
In Vivo

B10 (20-60 mg/kg; i.p.; every other day; 28 days) exhibits potent in vivo antitumor efficacy in a Huh-7 xenograft model, with a 64.18% TGI rate at 40 mg/kg, and maintains a favorable safety profile[1].

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

Animal Model: Balb/c nude mice (female, 4-6 weeks old, 18-19 g average weight)[1]
Dosage: 20, 40, 60 mg/kg; 40 mg/kg (TGI assessment)
Administration: i.p.; every other day; 28 days
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.
Molecular Weight

449.65

Formula

C27H35N3OS
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FGFR3-IN-11 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FGFR3-IN-11FGFRFibroblast growth factor receptorFGFR3/PI3K/AKT signaling pathwayhepatocytesxenograft mouse modelsFibroblast growth factor receptor 3Huh-7HepG2G0/G1 cell cycle arrestapoptosisMHCC97-Hhepatocellular carcinomaInhibitorinhibitorinhibit

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