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DGY-09-192 | DGY-09-192 : Degrader (PROTAC) of FGFR1, FGFR2
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
FGFR1
  • IC50:23.8 nM
  • DC50:4.35 nM
  • Dmax:85%
  • IC50:17 nM
FGFR2
  • IC50:34 nM
  • DC50:70 nM
  • Dmax:74%
  • IC50:1 nM
1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
In quantitative mass spectrometry-based proteomics following 5h treatment in Kelly cells expressing ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
FGFR3 (IC50 : 50.9 nM) and FGFR4 (IC50 : 353 nM) in biochemical assay but does not degrade these 2 p ...

Potency
Cellular
In Vitro

FGFR1

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.202101328

FGFR2

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.202101328

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 5.45 h
Systemic clearance: 5.58 mL/min/Kg
Cmax: 1.60 uM
Tmax: 0.08 h
Area Under the Curve:: 2.94 uM*h
Volume of Distribution at Steady-State: 1.41 L/Kg

DOI Reference: 10.1002/anie.202101328

Dose: 3 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 4.25 h
Systemic clearance: 6.84 mL/min/Kg
Cmax: 1.49 uM
Tmax: 1.33 h
Area Under the Curve:: 7.33 uM*h

DOI Reference: 10.1002/anie.202101328

Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 5.10 h
Systemic clearance: 1550.77 mL/min/Kg
Cmax: 0.01 uM
Tmax: 1.67 h
Area Under the Curve:: 0.07 uM*h
Fb : 0.2

DOI Reference: 10.1002/anie.202101328

Negative Control Compounds

DGY-09-192-Neg
Notes: CellTiter-Glo assay: FGFR2 - IC50 = 77 nM (>70 fold DGY-09-192) FGFR1 - IC50 = 232 nM (>13 fold DGY-09-192)

Chemical Information

Molecular Formula C49H59Cl2N11O7S
SMILEs COc1cc(OC)c(Cl)c(/N=C(\O)N(C)c2cc(Nc3ccc(N4CCN(C/C(O)=N/[C@H](C(=O)N5C[C@H](O)C[C@H]5/C(O)=N\[C@H](C)c5ccc(-c6scnc6C)cc5)C(C)(C)C)CC4)cc3)ncn2)c1Cl
InChI InChI=1S/C49H59Cl2N11O7S/c1-28(30-9-11-31(12-10-30)44-29(2)54-27-70-44)55-46(65)35-21-34(63)24-62(35)47(66)45(49(3,4)5)57-40(64)25-60-17-19-61(20-18-60)33-15-13-32(14-16-33)56-38-23-39(53-26-52-38)59(6)48(67)58-43-41(50)36(68-7)22-37(69-8)42(43)51/h9-16,22-23,26-28,34-35,45,63H,17-21,24-25H2,1-8H3,(H,55,65)(H,57,64)(H,58,67)(H,52,53,56)/t28-,34-,35+,45-/m1/s1
Molecular weight 1015.37 Da
AlogP 8.830720000000005
HBond acceptors 18
HBond donors 5
Atoms 129
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

Vendors

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Expert Reviews

by SERP
(on 4 Jan 2023)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 30 Jan 2023)
Cellular Use Rating
In Model Organisms
Also degrades PDE6D
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