TYRA-300 |
TYRA-300 : Inhibitor of FGFR3
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, G380R, N540K) |
|
|
Inhibitor
up to 100 nM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity of TYRA-300 for the human kinome was assessed with a KINOMEscan (Eurofins, San Diego, CA ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
In BaF3 cellular assay TYRA-300 showed to be selective for FGFR3 against FGFR1, 2, and 4.
Potency Cellular
In Vitro
FGFR3
(Mutant:WT, G380R, N540K)
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.4c01531
In Vivo Validations
Rat
Dose: 2 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.93 h
Systemic clearance:
17.5 mL/min/Kg
Area Under the Curve::
1734 h·ng/mL
Volume of Distribution at Steady-State:
2.5 L/Kg
DOI Reference: 10.1021/acs.jmedchem.4c01531
Dose: 10 mg/Kg
Route of delivery:
Oral
Cmax:
802 ± 198 ng/mL
Tmax:
4 h
Area Under the Curve::
3355 ±892h·ng/mL
Bioavailability:
39 ± 10%
DOI Reference: 10.1021/acs.jmedchem.4c01531
Dog
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
5.52 ± 0.34 h
Systemic clearance:
2.68 ± 0.15 mL/min/kg
Area Under the Curve::
5930 ± 298 h·ng/mL
Volume of Distribution at Steady-State:
1.12 ± 0.05 L/Kg
DOI Reference: 10.1021/acs.jmedchem.4c01531
Dose: 10 mg/Kg
Route of delivery:
Oral
Plasma half life:
24.8 h
Cmax:
ng/mL
Tmax:
6.0 ± 1.6 h
Area Under the Curve::
58300 ± 1810 h·ng/mL
Bioavailability:
98 ± 3%
DOI Reference: 10.1021/acs.jmedchem.4c01531
Monkey (Cynomolgus)
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.17 ± 0.15 h
Systemic clearance:
11.07 ± 0.66 mL/min/kg
Area Under the Curve::
1500 ± 86 h·ng/mL
Volume of Distribution at Steady-State:
0.94 ± 0.12 L/Kg
DOI Reference: 10.1021/acs.jmedchem.4c01531
Dose: 10 mg/Kg
Route of delivery:
Oral
Cmax:
1210 ± 742 ng/mL
Tmax:
6.0 h
Area Under the Curve::
15900 ± 8080 h·ng/mL
Bioavailability:
106 ± 54 %
DOI Reference: 10.1021/acs.jmedchem.4c01531
Chemical Information
| Molecular Formula | C25H24Cl2N6O3S |
| SMILEs | C[C@@H](Oc1ccc2[nH]nc(-c3ccc(N4CC5(C4)CN(S(C)(=O)=O)C5)nc3)c2c1)c1c(Cl)cncc1Cl |
| InChI | InChI=1S/C25H24Cl2N6O3S/c1-15(23-19(26)9-28-10-20(23)27)36-17-4-5-21-18(7-17)24(31-30-21)16-3-6-22(29-8-16)32-11-25(12-32)13-33(14-25)37(2,34)35/h3-10,15H,11-14H2,1-2H3,(H,30,31)/t15-/m1/s1 |
| Molecular weight | 558.10 Da |
| AlogP | 4.548300000000004 |
| HBond acceptors | 9 |
| HBond donors | 1 |
| Atoms | 61 |
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