1. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  2. PROTACs EGFR Apoptosis
  3. PROTAC EGFR degrader 5

PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase.

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PROTAC EGFR degrader 5 Chemical Structure

PROTAC EGFR degrader 5 Chemical Structure

CAS No. : 2409793-36-6

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Description

PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].

IC50 & Target

EGFR

34.8 nM (DC50)

In Vitro

PROTAC EGFR degrader 5 (PROTAC 10, 0-10 μM approximately, 72 h) inhibits HCC827 cell (NSCLC cell) proliferation with an IC50 value of 0.22 μM[1].
PROTAC EGFR degrader 5 (1 nM-10 μM, 48 h or 4-96 h) concentration-dependently and time-dependently degrades EGFR with a DC50 value of 34.8 nM in HCC827 cells[1].
PROTAC EGFR degrader 5 (0.1-1 μM, 36 h) concentration-dependently inhibits EGFR and downstream Akt phosphorylation in HCC827 cells[1].
PROTAC EGFR degrader 5 (0.1-10 μM, 48 h) displays weak degradation activity on EGFR in H1975 and A549 cells[1].
PROTAC EGFR degrader 5 (0.1-1 μM, 32 h) dose-dependently induces the apoptosis of HCC827 cells and arrests the cells in G1 phase[1].

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

Cell Proliferation Assay[1]

Cell Line: HCC827, H1975, A549, A431
Concentration: 0-10 μM approximately
Incubation Time: 72 h
Result: Displayed more potent anti-proliferative activity against HCC827 cells than other cells, IC50 values: 0.22 μM (HCC827), > 10μM (H1975, A549, A431), respectively.

Western Blot Analysis[1]

Cell Line: HCC827 cell
Concentration: 1 nM-10 μM
Incubation Time: 48h for concentration-dependent assay, 4-96 h for time-dependent assay
Result: Degraded EGFR with a DC50 value of 34.8 nM in HCC827 cell in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: HCC827 cell
Concentration: 0.1 μM, 1 μM
Incubation Time: 32 h
Result: Induced cell apoptosis in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HCC827 cell
Concentration: 0.1 μM, 1 μM
Incubation Time: 32 h
Result: Induced cell cycle arrest in G1 phase.
Molecular Weight

1070.33

Formula

C57H72FN13O5S

CAS No.
SMILES

CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCN4CCN(CC4)C5=CC=C(N=C5)NC6=NC=C7N=C(N=C(C7=C6)N8CCC(CC8)CO)NC9=CC=C(C=C9)F)=O)=O)O)=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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PROTAC EGFR degrader 5
Cat. No.:
HY-146422
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