PROTAC c-Met degrader-3
PROTAC c-Met degrader-3 is a c-Met PROTAC degrader with a DC50 of 0.59 nM. PROTAC c-Met degrader-3 induces ubiquitination and degradation of c-Met. PROTAC c-Met degrader-3 induces Apoptosis. PROTAC c-Met degrader-3 can be used in lung cancer-related research.
(Pink: c-Met ligand (HY-14721); Blue: Cereblon ligand (HY-W249500); Black: linker).
For research use only. We do not sell to patients.
- Formula: C51H54N10O7
- Molecular Weight:919.04
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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Cereblon |
c-Met 0.59 nM (DC50) |
PROTAC c-Met degrader-3 (Compound 22b) (0.03-1000 nM; 24 h) potently degrades c-Met in EBC-1 lung cancer cells, with a DC50 of 0.59 nM, and the maximum degradation rate reaches 96.14% at 15.6 nM[1].
PROTAC c-Met degrader-3 (15.6 nM; 3-72 h) induces time-dependent degradation of c-Met in EBC-1 lung cancer cells, with a maximum degradation rate of up to 93.13% after treatment at 15.6 nM for 72 h[1].
PROTAC c-Met degrader-3 potently inhibits the proliferation of c-Met-sensitive EBC-1 and Hs746T cancer cells, with IC50 values of 4 nM and 8 nM, respectively, while shows weak activity in c-Met-insensitive A549 and HCT116 cells[1].
PROTAC c-Met degrader-3 (3.9-15.6 nM; 7 days) significantly inhibits colony formation of EBC-1 lung cancer cells after 7 days of treatment at concentrations of 3.9, 7.8 and 15.6 nM[1].
PROTAC c-Met degrader-3 potently inhibits the proliferation of Tepotinib (HY-14721)-resistant MKN45 gastric cancer cells, with an IC50 value of 10 nM[1].
PROTAC c-Met degrader-3 (5-50 nM; 72 h) induces apoptosis in EBC-1 lung cancer cells, and mainly drives cells into the early apoptotic stage after treatment at 5, 15 or 50 nM for 72 h[1].
PROTAC c-Met degrader-3 (5-50 nM; 24 h) upregulates the expression of cleaved PARP and cleaved caspase-3 in EBC-1 lung cancer cells in a dose-dependent manner after 24 h of treatment, indicating that it induces apoptosis via these pathway markers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EBC-1 lung cancer cells
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Concentration:0.03-1000 nM
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Incubation Time:24 h
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Result:Dose-dependently degraded c-Met starting from 0.03 nM.
Achieved a maximum degradation rate (Dmax) of 96.14% at 15.6 nM.
Exhibited a DC50 of 0.59 nM.
Showed a hook effect at concentrations of 500 nM and 1000 nM.
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Cell Line:EBC-1 lung cancer cells
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Concentration:15.6 nM
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Incubation Time:3-72 h
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Result:Degraded c-Met in a time-dependent manner.
Reached maximal degradation (93.13%) at 72 h.
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Cell Line:EBC-1 lung cancer cells
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Concentration:5-50 nM
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Incubation Time:72 h
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Result:Induced apoptosis in EBC-1 cells.
Drove the majority of cells into early apoptosis at the tested concentrations.
| Species | Dose | Route | T1/2 | Tmax | C0 | Cmax | AUC0-t | AUC0-∞ | Vss | Vz | CL | MRT0-t | MRT0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 6.90 h | 0.0833 h | 1012.47 ng/mL | 2383.29 ng/mL | 531.98 ng·h/mL | 550.82 ng·h/mL | 36.26 L/kg | 13.13 L/kg | 60.78 mL/min/kg | 2.49 h | 3.58 h | / |
| Rat[1] | 5 mg/kg | i.p. | 5.49 h | 2.00 h | / | 104.35 ng/mL | 654.54 ng·h/mL | 677.67 ng·h/mL | / | / | / | 5.06 h | 6.00 h | 49.21 % |
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 mice (female, 4 weeks old, subcutaneous xenograft model via injection of 5×106 EBC-1 cells)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; once every 2 days
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Result:Reduced tumor volume by 60.28%.
Reduced tumor volume by 86.14%, which was superior to the equal dose of tepotinib (74.50% inhibition).
Showed no body weight loss in treated mice.
Exhibited no evident organ toxicity via H&E staining.
Induced dose-dependent tumor cell apoptosis and cell shrinkage via immunohistochemical analysis.
Chemical Information
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Molecular Weight 919.04
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Formula C51H54N10O7
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SMILES
O=C(N1)N(C2=CC(C(N3CCC4(CCN(CC4)C(CN5CCC(COC6=CN=C(N=C6)C7=CC=CC(CN8N=C(C=CC8=O)C9=CC(C#N)=CC=C9)=C7)CC5)=O)CC3)=O)=CC=C2OC)CCC1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)