DGY-09-192

DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM) . DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN) . DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers. (Pink: FGFR1/2 ligand (HY-160013), Blue: VHL Ligand (HY-112078), Black: Linker (HY-W020017) ) [1].

Product Specifications

CAS Number

[2504949-52-2]

UNSPSC

12352005

Target

ERK; FGFR; PROTACs

Related Pathways

MAPK/ERK Pathway; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer

Purity

99.50

Solubility

DMSO : ≥ 100 mg/mL

Smiles

ClC(C(OC)=CC(OC)=C1Cl)=C1NC(N(C)C2=CC(NC(C=C3)=CC=C3N(CC4)CCN4CC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(N[C@H](C6=CC=C(C7=C(N=CS7)C)C=C6)C)=O)=O)=O)=NC=N2)=O

Molecular Formula

C49H59Cl2N11O7S

Molecular Weight

1017.03

References & Citations

[1]Du G, et al. Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2. Angew Chem Int Ed Engl. 2021 Jul 12;60 (29) :15905-15911.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

FGFR1; FGFR2; von Hippel-Lindau (VHL)

Available Sizes

Curated Selection

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