2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs FGFR
  4. 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.

PROTAC FGFR3 Degrader-1

PROTAC FGFR3 Degrader-1 Chemical Structure

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PROTAC FGFR3 Degrader-1 Related Antibodies

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Description

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[1]. (Pink: FGFR3 ligand (HY-181152); Blue: Cereblon ligand (HY-14658); Black: linker).

In Vitro

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.

PROTAC FGFR3 Degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: Huh-7
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)
Incubation Time: 24 h (1 μM treatment; co-treatments)
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.

Western Blot Analysis[1]

Cell Line: Huh-7
Concentration: 0.25-1 μM (dose-dependent assessment); 1 μM (time-dependent assessment)
Incubation Time: 6 h, 12 h, 24 h (1 μM treatment)
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.
Molecular Weight

844.04

Formula

C46H53N9O5S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC FGFR3 Degrader-1 Related Classifications

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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:

PROTAC FGFR3 Degrader-1PROTACsFGFRFibroblast growth factor receptorFGFR3/PI3K/AKT signaling pathwayHuh-7HepG2PI3Kfibroblast growth factor receptor 3ubiquitin-proteasome pathwayMHCC97-Hproteasome pathwayFGFR3hepatocellular carcinomaInhibitorinhibitorinhibit

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