DGY-09-192

• Description:

  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].

• 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)

• CAS Number:

  2504949-52-2