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FGFR3-IN-10s | FGFR3-IN-10s : Covalent Inhibitor of FGFR3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FGFR3 (Mutant:WT, V555M)
  • IC50:6.8 nM
  • IC50:19.2 nM
  • IC50:9.2 nM
  • INH:80 nM
up to 500 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Compound 10s displayed promising FGFR3 selectivity in the cellular assays with an RT112/84 IC50 valu ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Compound 10s demonstrated improved selectivity over FGFR1/2 (43.5/5.3-fold)
In Vitro Selectivity Assessment
TNK1

Gene ID: Q13470

Organism: Homo sapiens

Family: Tyr protein kinase family

Potency: IC50 - 16.9 nM

Potency Assay Off-Target:
Kinase profiling of cpd 10s at a concentration of 0.5 μM was conducted against a panel of 330 wild-t ...
Selectivity Assessment Description:
Results demonstrated that cpd 10s displayed extraordinary kinome selectivity with S(1) and S(10) sel ...

Potency
Cellular
In Vitro

FGFR3 (Mutant:WT, V555M)

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5c02552

In Vivo Validations

Rat
Dose: 2 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.47 h
Systemic clearance: 133.4 mL/min/Kg
Cmax: 656 ng/mL
Tmax: 0.083 h
Area Under the Curve:: 249 h*ng/mL

DOI Reference: 10.1021/acs.jmedchem.5c02552

Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 0.59 h
Cmax: 69.3 ng/mL
Tmax: 0.25 h
Area Under the Curve:: 46.6 h*ng/mL
Bioavailability: 3.74%

DOI Reference: 10.1021/acs.jmedchem.5c02552

Chemical Information

Molecular Formula C26H30N8O2
SMILEs C=CC(=O)Nc1ccc2c(-c3ccnc(Nc4cnn(CCN5CCOCC5)c4C)n3)cn(C)c2c1
InChI InChI=1S/C26H30N8O2/c1-4-25(35)29-19-5-6-20-21(17-32(3)24(20)15-19)22-7-8-27-26(30-22)31-23-16-28-34(18(23)2)10-9-33-11-13-36-14-12-33/h4-8,15-17H,1,9-14H2,2-3H3,(H,29,35)(H,27,30,31)
Molecular weight 486.25 Da
AlogP 3.3405200000000015
HBond acceptors 10
HBond donors 2
Atoms 66

References

Publications

Cross References

canSAR: 7719214 canSAR: 17

Expert Reviews

by SERP
(on 7 Jun 2026)
Cellular Use Rating
In Model Organisms
Covalent FGFR3 inhibitor with off-target activity on TNK1, FGFR2 and to a lesser extent FGFR1/4. Otherwise clean profile. Note that covalent inhibition is time-dependent, with potency increasing with incubation...
by SERP+
(on 9 Jul 2026)
Cellular Use Rating
In Model Organisms
The probe is a potent, selective, low nanomolar inhibitor for FGFR3 with a 50-fold selectivity over FGFR1. When screened against the kinome at 0.5uM, the probe showed potency against TNK1 (16.9nM). Cocrystal...
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