PROTAC FGFR3 Degrader-1
PROTAC FGFR3 Degrader-1 is a fibroblast growth factor receptor 3 (FGFR3) PROTAC degrader, promotes FGFR3 degradation via the ubiquitin-proteasome pathway, and inhibits the downstream FGFR3/PI3K/AKT signaling pathway. PROTAC FGFR3 Degrader-1 can be used for the research of hepatocellular carcinoma.
(Pink: FGFR3 ligand (HY-181152); Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- Formula: C46H53N9O5S
- Molecular Weight:844.04
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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- References
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Biological Activity
PROTAC FGFR3 Degrader-1 (48 h) potently inhibits the proliferation of Huh-7, HepG2, and MHCC97-H hepatocellular carcinoma cells with IC50 values of 0.56 μM, 1.44 μM, and 1.87 μM, respectively[1].
PROTAC FGFR3 Degrader-1 (0.125-1 μM; 24 h) promotes dose-dependent degradation of FGFR3 protein in Huh-7 cells via the proteasome pathway, and this degradation is inhibited by B10 or pomalidomide co-treatment[1].
PROTAC FGFR3 Degrader-1 (0.25-1 μM; 6-24 h) downregulates FGFR3 expression and inhibits FGFR3/PI3K/AKT signaling pathway activity in a time- and dose-dependent manner in Huh-7 cells[1].
PROTAC FGFR3 Degrader-1 (40 μM) stably binds to FGFR3 in Huh-7 cells, as demonstrated by its ability to protect FGFR3 from thermal denaturation in a cellular thermal shift assay[1].
PROTAC FGFR3 Degrader-1 (10-40 μM) stably binds to FGFR3 in Huh-7 cell lysates, as shown by its dose-dependent protection of FGFR3 from pronase digestion in a drug affinity responsive target stability assay[1].
PROTAC FGFR3 Degrader-1 stably binds to FGFR3 with a binding energy of -7.5 kcal/mol, as predicted by molecular docking[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh-7
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Concentration:0.125-1 μM (degradation efficiency assessment); 1 μM (24 h treatment alone); 10 μM MG132 (co-treatment); 1 μM B10 (co-treatment); 10 μM pomalidomide (co-treatment)
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Incubation Time:24 h (1 μM treatment; co-treatments)
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Result:Promoted dose-dependent degradation of FGFR3 protein, with significant degradation observed at 0.5 μM and 1 μM. Had its induced FGFR3 degradation rescued by co-treatment with MG132, had its induced FGFR3 degradation inhibited by co-treatment with its precursor B10, and had its induced FGFR3 degradation inhibited by co-treatment with the CRBN E3 ligase ligand pomalidomide.
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Cell Line:Huh-7
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Concentration:0.25-1 μM (dose-dependent assessment); 1 μM (time-dependent assessment)
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Incubation Time:6 h, 12 h, 24 h (1 μM treatment)
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Result:Downregulated FGFR3 expression and inhibited PI3K/AKT pathway activity in a time- and dose-dependent manner. Had its induced suppression of PI3K/AKT pathway activity significantly reversed by activation of FGFR3.
Chemical Information
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Molecular Weight 844.04
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Formula C46H53N9O5S
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SMILES
O=C(C1=CC2=C(N3C[C@@]4(CCCN5CCC[C@@]([C@@]54[H])([C@]3(CC2)[H])[H])[H])S1)NC6=C(C7=CN(CCCCNC8=CC=CC(C(N9C%10CCC(NC%10=O)=O)=O)=C8C9=O)N=N7)C=C(C(C)C)C=C6
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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)
PROTAC FGFR3 Degrader-1 Related Classifications
HY-181153 Related Classifications
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