PROTAC FGFR2 degrader 1
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker: HY-163986) [1].
Product Specifications
CAS Number
[3099123-99-3]
UNSPSC
12352005
Target
Apoptosis; FGFR; PROTACs
Type
Reference compound
Related Pathways
Apoptosis; PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/protac-fgfr2-degrader-1.html
Smiles
COC1=CC(OC)=CC(N(C2=CC=C3N=CC(C4=CN(N=C4)CCCCCCC(NCCNC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=NC3=C2)CCNC(C)C)=C1
Molecular Formula
C46H54N10O7
Molecular Weight
858.98
References & Citations
[1]Zhanzhan Feng, et al. Synthesis and identification of a selective FGFR2 degrader with potent
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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