2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FGFR TNK1 Apoptosis Caspase
  4. 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.

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FGFR3-IN-12

FGFR3-IN-12 Chemical Structure

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FGFR3-IN-12 Related Antibodies

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Description

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[1].

IC50 & Target[1]

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

 

In Vitro

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.

FGFR3-IN-12 Related Antibodies

Western Blot Analysis[1]

Cell Line: RT112/84 bladder carcinoma cells, Ba/F3-FGFR3V555M engineered cells
Concentration: 6.25-100 nM (RT112/84 cells); 5-80 nM (Ba/F3-FGFR3V555M cells)
Incubation Time: 48 h (RT112/84 cells); 6 h (Ba/F3-FGFR3V555M cells)
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.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast AUC0-inf F CL
Rat[1] 2.0 mg/kg i.v. 0.47 h 0.083 h 656 ng/mL 249 ng·h/mL 251 ng·h/mL / 133.4 mL/min/kg
Rat[1] 10.0 mg/kg p.o. 0.59 h 0.25 h 69.3 ng/mL 46.6 ng·h/mL 47.07 ng·h/mL 3.74 % /
In Vivo

FGFR3-IN-12 (Compound 10s) (20-40 mg/kg; i.p.; daily for 15 days) exhibits dose-dependent antitumor efficacy in RT112/84 bladder cancer xenografts in nude mice, achieving a maximum tumor growth inhibition of 77.1% at 40 mg/kg with no significant observed toxicity[1].

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

Animal Model: BALB/C nude with RT112/84 bladder cancer xenografts (female, 4 weeks old)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: I.p.; daily for 15 days
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.
Molecular Weight

486.57

Formula

C26H30N8O2
SMILES

CN1C2=C(C(C3=NC(NC4=C(N(N=C4)CCN5CCOCC5)C)=NC=C3)=C1)C=CC(NC(C=C)=O)=C2
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-12 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-12FGFRTNK1ApoptosisCaspaseFibroblast growth factor receptorTyrosine kinase non receptor 1KOS1bladder cancer cellsFGFR4bladder cancerFGFR2FGFR1RT112/84 bladder carcinoma cellsFGFR3 V555MFGFR3bladder cancer xenograft modelsInhibitorinhibitorinhibit

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