PROTAC c-Met degrader-1
Based on 1 Customer Validation
PROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC50 of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer.
(Pink: c-Met ligand (HY-13404); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W074901)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.48%
- CAS. Nr.: 3056647-52-7
- Formel: C45H41FN10O5
- Molecular Weight:820.87
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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c-Met 6.21 nM (DC50) |
In Vitro
PROTAC c-Met degrader-1 (Met-DD4) (0.1954-200 nM; 1-24 h) potently and dose-dependently degrades c-Met in MKN-45 cells with a DC50 of 6.21 nM, achieving 96.83% maximal degradation and time-dependent degradation that peaks at 16 h[1].
PROTAC c-Met degrader-1 (72 h) potently inhibits the proliferation of c-Met-addicted MKN-45 cells with an IC50 of 4.37 nM[1].
PROTAC c-Met degrader-1 induces robust c-Met degradation and blocks c-Met-Akt signaling in Hs746T and PC-9 cells[1].
PROTAC c-Met degrader-1 (100 nM; 1-24 h) induces c-Met degradation in MKN-45 cells via a CRBN-mediated ubiquitin-proteasome pathway[1].
PROTAC c-Met degrader-1 (100 nM; 24 h) exhibits high degradation selectivity for c-Met in MKN-45 cells, with no other proteins significantly downregulated more than 4-fold[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MKN-45
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Concentration:100 nM
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Incubation Time:1 h, 2 h, 3 h, 4 h, 8 h,16 h, 24 h
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Result:Had c-Met degradation significantly reversed by pretreatment with 5 μM capmatinib, 10 μM pomalidomide, 5 μM MG132, or 5 μM MLN4924.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female) injected with MKN-45 cells[1]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Exhibited dose-dependent tumor growth retardation.
Induced degradation of total and phosphorylated c-Met in tumor tissues compared to vehicle control at all three doses.
Caused no significant body weight loss in any treated group.
Showed normal organ morphology in lung, liver, spleen, kidney, and heart with no evidence of systemic toxicity.
Chemical Information
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CAS. Nr. 3056647-52-7
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Appearance Solid
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Molecular Weight 820.87
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Formel C45H41FN10O5
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Color Light yellow to yellow
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SMILES
FC1=C(C=CC(C(C=N2)=NN3C2=NC=C3CC4=CC5=C(C=C4)N=CC=C5)=C1)C(N6CCC(CN7CCN(C8=CC9=C(C=C8)C(N(C9=O)C(C(N%10)=O)CCC%10=O)=O)CC7)CC6)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (121.82 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (278 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)
Verweise
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 | 1.2182 mL | 6.0911 mL | 12.1822 mL | 30.4555 mL |
| 5 mM | 0.2436 mL | 1.2182 mL | 2.4364 mL | 6.0911 mL | |
| 10 mM | 0.1218 mL | 0.6091 mL | 1.2182 mL | 3.0455 mL | |
| 15 mM | 0.0812 mL | 0.4061 mL | 0.8121 mL | 2.0304 mL | |
| 20 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5228 mL | |
| 25 mM | 0.0487 mL | 0.2436 mL | 0.4873 mL | 1.2182 mL | |
| 30 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 40 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 50 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6091 mL | |
| 60 mM | 0.0203 mL | 0.1015 mL | 0.2030 mL | 0.5076 mL | |
| 80 mM | 0.0152 mL | 0.0761 mL | 0.1523 mL | 0.3807 mL | |
| 100 mM | 0.0122 mL | 0.0609 mL | 0.1218 mL | 0.3046 mL |
PROTAC c-Met degrader-1 Related Classifications
HY-168135 Related Classifications
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