2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR4-IN-24

FGFR4-IN-24 is a selective irreversible covalent FGFR4 inhibitor (IC50 = 1.2 nM). FGFR4-IN-24 shows much weaker activity against the other three FGFR family kinases (FGFR1-3). FGFR4-IN-24 inhibits the FGF19/FGFR4 signaling pathway, effectively suppressing the proliferation of the HuH-7 HCC cell line (GI50 = 17 nM). FGFR4-IN-24 exhibits significant antitumor activity in a HuH-7 mouse xenograft model. FGFR4-IN-24 can be used for the research of hepatocellular carcinoma.

For research use only. We do not sell to patients.

FGFR4-IN-24

FGFR4-IN-24 Chemical Structure

CAS No. : 3053546-73-6

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FGFR4-IN-24 Related Antibodies

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Description

FGFR4-IN-24 is a selective irreversible covalent FGFR4 inhibitor (IC50 = 1.2 nM). FGFR4-IN-24 shows much weaker activity against the other three FGFR family kinases (FGFR1-3). FGFR4-IN-24 inhibits the FGF19/FGFR4 signaling pathway, effectively suppressing the proliferation of the HuH-7 HCC cell line (GI50 = 17 nM). FGFR4-IN-24 exhibits significant antitumor activity in a HuH-7 mouse xenograft model. FGFR4-IN-24 can be used for the research of hepatocellular carcinoma[1].

IC50 & Target[1]

FGFR4

1.2 nM (IC50)

In Vitro

FGFR4-IN-24 (Compound 10v) (3 nmol/L, 0-30 min) shows a time-dependent enhancement in apparent inhibitory activity with prolonged preincubation, consistent with its ability to covalently modify FGFR4[1].
FGFR4-IN-24 (kinact/KI = 4.8 × 105 M-1s-1) exhibits superior potency, mainly due to its tighter binding to FGFR4 kinase (KI = 0.62 nM) from a binding mode that boosts noncovalent affinity[1].
FGFR4-IN-24 (72 h) inhibits the proliferation of HuH-7 cell line (IC50 = 1.2 nM, GI50 = 17 nM)[1].
FGFR4-IN-24 (1 μM) exhibits substantial inhibition of FGFR4 (79%) with high selectivity[1].
FGFR4-IN-24 (1-1000 nM, 2 h) inhibits the phosphorylation of the FGFR4 substrate FRS2α and reduces the phosphorylation levels of ERK in HuH-7 cells[1].

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

FGFR4-IN-24 Related Antibodies

Cell Viability Assay[1]

Cell Line: HuH-7 cells
Concentration:
Incubation Time: 72 h
Result: Induced a growth inhibition 50% (GI50) of 17 nM.

Western Blot Analysis[1]

Cell Line: HuH-7 cells
Concentration: 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 2 h
Result: Inhibited almost completely the phosphorylation of FRS2α at 100 nM.
Reduced the phosphorylation levels of ERK.
Maintained the inhibition of FRS2α and ERK phosphorylation at 300 nM even after extensive washing with phosphate-buffered saline (PBS) (HY-K3005).
Parmacokinetics
Species Dose Route T1/2 MRT Vz Vss CL Cmax AUC0-t AUC0-∞ Bioavailability Tmax
Mice[1] 2 mg/kg i.v. 0.5 h 0.3 h 0.37 L/kg 0.15 L/kg 8.28 mL/min/kg 17449 ng/mL 4143 ng·h/mL 4147 ng·h/mL / /
Mice[1] 5 mg/kg i.p. 12.7 h 4.87 h / / / 2377 ng/mL 10331 ng·h/mL 12421 ng·h/mL 120 % 0.83 h
Mice[1] 5 mg/kg p.o. 0.98 h 0.74 h / / / 65.8 ng/mL 55.2 ng·h/mL 75.4 ng·h/mL 0.73 % 0.25 h
In Vivo

FGFR4-IN-24 (Compound 10v) (25, 50 mg/kg, i.p., twice a day for 21 days) suppresses tumor growth in a dose-dependent manner and maintains the body weight in HuH-7 xenograft mouse model[1].

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

Animal Model: HuH-7 xenograft mouse model in female BALB/c nude mice (4 weeks)[1]
Dosage: 25, 50 mg/kg
Administration: Intraperitoneal administration (i.p.), twice daily for 21 days
Result: Significantly inhibited tumor growth at 25 mg/kg, with a tumor growth inhibition (TGI) ratio of 85%.
Caused tumor regression at 50 mg/kg, with a TGI ratio of 114%.
Induced no significant reduction in body weight.
Molecular Weight

483.49

Formula

C27H22FN5O3
CAS No.
SMILES

C=CC(NC1=CC=CC=C1NC2=CC=C(C(C(C3=C(F)C=CC(C(NC4CC4)=O)=C3)=O)=CN5)C5=N2)=O
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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FGFR4-IN-24 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:

FGFR4-IN-243053546-73-6FGFRFibroblast growth factor receptorFibroblast growth factor receptor 4Irreversible covalent inhibitorHepatocellular carcinomaInhibitorinhibitorinhibit

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