1. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Membrane Transporter/Ion Channel
  2. PROTACs EGFR ATP Synthase
  3. PROTAC EGFR degrader 15

PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737)).

For research use only. We do not sell to patients.

PROTAC EGFR degrader 15

PROTAC EGFR degrader 15 Chemical Structure

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Description

PROTAC EGFR degrader 15 is a Pomalidomide (HY-10984)-based Gefitinib (HY-50895) EGFR PROTAC degrader. PROTAC EGFR degrader 15 triggers EGFR degradation via ubiquitin-proteasome-dependent proteolysis and autophagy-lysosome activation pathways. PROTAC EGFR degrader 15 targets ETFA to enhance ATP production. PROTAC EGFR degrader 15 significantly suppresses tumor growth in a Gefitinib-acquired resistant HCC-827 xenograft model. PROTAC EGFR degrader 15 can be used for the study of non-small cell lung cancer (NSCLC) (Pink: EGFR ligand (HY-W109039); Blue: CRBN ligand (HY-10984); Black: Linker (HY-W679737))[1].

IC50 & Target[1]

Cereblon

 

In Vitro

PROTAC EGFR degrader 15 (Compound P-G) (0-1 μM, 24 h + washout 0-72 h) effectively and sustainably induces EGFR protein degradation via both ubiquitin/proteasome pathway and autophagy/lysosome degradation pathway both in HCC-827 parental and EGFR-tyrosine kinase inhibitors (EGFR-TKIs) resistant cells[1].
PROTAC EGFR degrader 15 (0.5 μM, 44-64°C, 2 h) promotes energy production in HCC-827-ER (Erlotinib (HY-50896) resistance) resistance cells by targeting ETFA[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HCC-827, HCC-827-GR, HCC-827-ER, HCC-827-OR and HCC-827-RR cells
Concentration: 0, 0.1, 0.5 and 1 μM
Incubation Time: 24 h + washout 0, 6, 12, 24, 48 and 72 h
Result: Exhibited concentration-dependent and long lasting degradation of EGFR and p-EGFR in all cell lines.

Western Blot Analysis[1]

Cell Line: HCC-827 cells
Concentration: 0.5 μM
Incubation Time: 2 h
Result: Resulted in a significant increase in the thermal stability of ETFA at various temperatures both in intact cells.
In Vivo

PROTAC EGFR degrader 15 (Compound P-G) (30 mg/kg, i.p., every other day for 2 weeks) effectively suppresses HCC-827-GR xenografts tumors in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HCC-827-GR xenografts model established in male BALB/c nude mice (20 g)[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.), every other day for 2 weeks
Result: Suppressed the HCC-827-GR xenografts tumor and the tumor growth inhibition (TGI) was 48.24 %.
Were no statistical differences in organ indices between vehicle treated group.
Molecular Weight

871.40

Formula

C45H52ClFN8O7

SMILES

O=C(N1)CCC(N2C(C(C(NC(CCCCCCCCCN3CCN(CCCOC4=CC(C(NC5=CC(Cl)=C(F)C=C5)=NC=N6)=C6C=C4OC)CC3)=O)=CC=C7)=C7C2=O)=O)C1=O

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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  • 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.

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Product Name:
PROTAC EGFR degrader 15
Cat. No.:
HY-175839
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