Chemical Probes logo
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
Download

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
Degrader (PROTAC)
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 0.0
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

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 4 Jan 2023 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 30 Jan 2023 )
Cellular Use Rating
In Model Organisms
Also degrades PDE6D
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria