DGY-09-192
Based on 1 Customer Validation
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 and FGFR2 ligand (HY-160013); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.50%
- CAS No.: 2504949-52-2
- Formula: C49H59Cl2N11O7S
- Molecular Weight:1017.03
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
|
VHL |
FGFR1 4.35 nM (DC50) |
FGFR2 70 nM (DC50) |
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.
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Cell Line:CCLP1-FP cells
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Concentration:50 nM
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Incubation Time:4, 8 h
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Result:Suppressed the phosphorylation of FRS2 at Y196 and ERK1/2 at T202/Y204.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:20 mg/kg and 40 mg/kg
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Administration:i.p., once daily, 6 days
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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.
Chemical Information
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CAS No. 2504949-52-2
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Appearance Solid
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Molecular Weight 1017.03
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Formula C49H59Cl2N11O7S
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Color White to off-white
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- 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)
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Handling Instructions (2659 KB)
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 |
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| 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 |
DGY-09-192 Related Classifications
HY-165298 Related Classifications
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