DGY-09-192

DGY-09-192 : Degrader (PROTAC) of FGFR1, FGFR2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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.

Probe DGY-09-192 is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Information

FGFR1
FGFR2

Degrader (PROTAC)

1 uM

Probe Availability:

ProbeChem

In Vitro Validations

Uniprot ID: P11362

Target Class: Kinase

Target SubClass: TK

Potency: IC50

Potency Value: 23.8 nM

Potency Assay: Z’-LYTE kinase assay by Invitrogen

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Fibroblast growth factor receptor 1, HBGFR, FLT2, ...

DOI Reference: 10.1002/anie.202101328

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): In quantitative mass spectrometry-based proteomics following 5h treatment in Kelly cells expressing both FGFR1 and FGFR2, DGY-09-192 exhibited a high selectivity for FGFR1 and FGFR2 with PDE6D as an off-target.

Potency assay (off target): FGFR3 (IC50 : 50.9 nM) and FGFR4 (IC50 : 353 nM) in biochemical assay but does not degrade these 2 proteins

I have extra information to add

SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 4 Jan 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

Also degrades PDE6D

(last updated: 30 Jan 2023 )