2. PROTAC Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway
  3. PROTACs FGFR ERK
  4. 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)).

For research use only. We do not sell to patients.

DGY-09-192

DGY-09-192 Chemical Structure

CAS No. : 2504949-52-2

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DGY-09-192 Related Antibodies

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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].

IC50 & Target[1]

VHL

 

FGFR1

4.35 nM (DC50)

FGFR2

70 nM (DC50)

In Vitro

DGY-09-192 (0.01-10 μM, 6 h) induces dose-dependent degradation of FGFR2 in KATO III cells, with a DC50 of 70 nM and a Dmax of 74%[1].
DGY-09-192 (0.1-1 μM, 24 h) leads to dose-dependent degradation of FGFR2-PHGDH fusion protein in CCLP-1-FP cells (with ectopic expression of FGFR2-PHGDH fusion) and FGFR2-OPTN fusion protein in ICC13-7 cells (with endogenous expression of FGFR2-OPTN fusion)[1].
DGY-09-192 (0.1-10 μM, 16 h) effectively degrades FGFR1 in CCLP1 cells (with FGFR1 overexpression) with a DC50 of 4.35 nM and a Dmax of 85%[1].
DGY-09-192 (0.0001-100000 nM, 72 h) shows anti-proliferative activities against KATO III cells (IC50 = 1 nM), CCLP1 cells (IC50 = 17 nM), ICC13-7 cells (IC50 = 40 nM) and CCLP-FP cells (IC50 = 8 nM)[1].
DGY-09-192 (50 nM, 4-8 h) durably suppresses downstream FGFR2 signaling in CCLP1-FP cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DGY-09-192 Related Antibodies

Western Blot Analysis[1]

Cell Line: CCLP1-FP cells
Concentration: 50 nM
Incubation Time: 4, 8 h
Result: Suppressed the phosphorylation of FRS2 at Y196 and ERK1/2 at T202/Y204.
In Vivo

DGY-09-192 (20-40 mg/kg, i.p., once daily, 6 days) induces reduction in FGFR2-PHGDH fusion protein levels and phosphorylation of downstream markers FRS2 (Y196) and ERK1/2 (T202/Y204) in CCLP1-FGFR2-PHGDH xenograft tumor model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CCLP1-FGFR2-PHGDH xenograft tumor model: CCLP1 cells with ectopic expression of FGFR2-PHGDH fusion protein were used to establish xenograft tumors[1]
Dosage: 20 mg/kg and 40 mg/kg
Administration: i.p., once daily, 6 days
Result: Induced dose-dependent reduction in FGFR2-PHGDH fusion protein levels in tumor tissues.
Caused dose-dependent decrease in phosphorylation of downstream signaling markers FRS2 (Y196) and ERK1/2 (T202/Y204) in tumor tissues.
Molecular Weight

1017.03

Formula

C49H59Cl2N11O7S
CAS No.
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
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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DGY-09-192 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DGY-09-1922504949-52-2PROTACsFGFRERKFibroblast growth factor receptorExtracellular signal regulated kinasesFGFR1/2PROTACICC13-7 cellsCCLP-1-FP cellsKATO III cellsInhibitorinhibitorinhibit

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