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

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

DGY-09-192 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast CL Vss F
Mice[1] 1 mg/kg i.v. 5.45 h 0.08 h 1.60 μM 2.94 μM·h 5.58 mL/min/kg 1.41 L/kg /
Mice[1] 10 mg/kg p.o. 5.10 h 1.67 h 0.01 μM 0.07 μM·h 1550.77 mL/min/kg / 20 %
Mice[1] 3 mg/kg i.p. 4.25 h 1.33 h 1.49 μM 7.33 μM·h 6.84 mL/min/kg / /
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.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (98.33 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9833 mL 4.9163 mL 9.8326 mL
5 mM 0.1967 mL 0.9833 mL 1.9665 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9833 mL 4.9163 mL 9.8326 mL 24.5814 mL
5 mM 0.1967 mL 0.9833 mL 1.9665 mL 4.9163 mL
10 mM 0.0983 mL 0.4916 mL 0.9833 mL 2.4581 mL
15 mM 0.0656 mL 0.3278 mL 0.6555 mL 1.6388 mL
20 mM 0.0492 mL 0.2458 mL 0.4916 mL 1.2291 mL
25 mM 0.0393 mL 0.1967 mL 0.3933 mL 0.9833 mL
30 mM 0.0328 mL 0.1639 mL 0.3278 mL 0.8194 mL
40 mM 0.0246 mL 0.1229 mL 0.2458 mL 0.6145 mL
50 mM 0.0197 mL 0.0983 mL 0.1967 mL 0.4916 mL
60 mM 0.0164 mL 0.0819 mL 0.1639 mL 0.4097 mL
80 mM 0.0123 mL 0.0615 mL 0.1229 mL 0.3073 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

DGY-09-192 Related Classifications

Help & FAQs
  • 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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
DGY-09-192
Cat. No.:
HY-165298
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Korean - KR (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.