FGFR3-IN-12
FGFR3-IN-12 is a selective fibroblast growth factor receptor 3 (FGFR3) inhibitor with an IC50 of 6.8 nM. FGFR3-IN-12 shows an IC50 of 19.2 nM against FGFR3V555M and an IC50 of 16.9 nM against TNK1 (Thirty-eight Negative Kinase 1). FGFR3-IN-12 inhibits cancer cells proliferation and induces caspase-mediated apoptosis. FGFR3-IN-12 exhibits antitumor activity in bladder cancer xenografts mice models. FGFR3-IN-12 can be used for the research of cancer, such as bladder cancer.
For research use only. We do not sell to patients.
- CAS No.: 3127143-52-3
- Formula: C26H30N8O2
- Molecular Weight:486.57
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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
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- References
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Biological Activity
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FGFR3 6.8 nM (IC50) |
FGFR3V555M 19.2 nM (IC50) |
FGFR2 35.7 nM (IC50) |
FGFR1 296.2 nM (IC50) |
FGFR4 414.5 nM (IC50) |
Caspase-3 |
Caspase-7 |
FGFR3-IN-12 (Compound 10s) potently inhibits wild-type FGFR3 with an IC50 of 6.8 nM, and exhibits 5 to 60-fold selectivity over wild-type FGFR1, FGFR2, and FGFR4[1].
FGFR3-IN-12 (30 min) inhibits the FGFR3V555M mutant with an IC50 of 19.2 nM[1].
FGFR3-IN-12 (5 days) potently inhibits proliferation of FGFR3-driven RT112/84 bladder carcinoma cells with an IC50 of 9.2 nM, and exhibits 3.2- to 48.6-fold selectivity over FGFR1-amplified, FGFR2-mutant, and FGFR4-mutant cancer cell lines[1].
FGFR3-IN-12 (0.5 μM) displays extraordinary kinome selectivity and potently inhibits TNK1 with an IC50 of 16.9 nM[1].
FGFR3-IN-12 (1 h) covalently binds to recombinant FGFR3, forming an adduct after 1 h incubation at a 1:2 (FGFR3:FGFR3-IN-12) molar ratio[1].
FGFR3-IN-12 (2 h) covalently modifies the Cys482 residue in the FGFR3 kinase domain after 2 h incubation at a 1:5 (FGFR3:FGFR3-IN-12) molar ratio[1].
FGFR3-IN-12 (6.25-100 nM; 6-48 h) concentration-dependently inhibits FGFR3 signaling and induces apoptosis in RT112/84 bladder carcinoma cells and inhibits FGFR3V555M signaling in engineered Ba/F3 cells[1].
FGFR3-IN-12 (20-80 nM; 96 h) concentration-dependently activates Caspase-3/7 in RT112/84 bladder carcinoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RT112/84 bladder carcinoma cells, Ba/F3-FGFR3V555M engineered cells
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Concentration:6.25-100 nM (RT112/84 cells); 5-80 nM (Ba/F3-FGFR3V555M cells)
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Incubation Time:48 h (RT112/84 cells); 6 h (Ba/F3-FGFR3V555M cells)
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Result:Caused a concentration-dependent reduction in phosphorylated FGFR3, phosphorylated ERK, and phosphorylated AKT in RT112/84 cells, with no change in total FGFR3, ERK, or AKT levels.
Induced concentration-dependent cleavage of PARP and activation of Caspase-7 in RT112/84 cells.
Caused a concentration-dependent reduction in phosphorylated FGFR3, phosphorylated MAPK, and phosphorylated AKT in Ba/F3-FGFR3V555M cells, with no change in total FGFR3, MAPK, or AKT levels.
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 with RT112/84 bladder cancer xenografts (female, 4 weeks old)[1]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:I.p.; daily for 15 days
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Result:Achieved 43.5% tumor growth inhibition at 20 mg/kg.
Achieved 77.1% tumor growth inhibition at 40 mg/kg.
Reduced tumor weight significantly relative to controls at both doses, with greater efficacy at 40 mg/kg.
Caused no significant body weight loss (>10%) or overt toxicity during treatment.
Suppressed Ki-67 staining in a dose-dependent manner, indicating reduced tumor cell proliferation.
Chemical Information
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CAS No. 3127143-52-3
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Molecular Weight 486.57
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Formula C26H30N8O2
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SMILES
CN1C2=C(C(C3=NC(NC4=C(N(N=C4)CCN5CCOCC5)C)=NC=C3)=C1)C=CC(NC(C=C)=O)=C2
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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-12 Related Classifications
HY-181752 Related Classifications
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