1. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  2. PROTACs EGFR Apoptosis
  3. PROTAC EGFR degrader 6

PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase.

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PROTAC EGFR degrader 6 Chemical Structure

PROTAC EGFR degrader 6 Chemical Structure

CAS No. : 2409793-28-6

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Description

PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase[1].

IC50 & Target

IC50: 180 nM (EGFRDel19 in HCC827 cells)[1]
DC50: 45.2 nM (EGFRDel19 in HCC827 cells)[1]

Cellular Effect
Cell Line Type Value Description References
A-431 IC50
> 10 μM
Compound: 2
Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
A549 IC50
> 10 μM
Compound: 2
Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
HCC827 IC50
0.18 μM
Compound: 2
Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
NCI-H1975 IC50
> 10 μM
Compound: 2
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
In Vitro

PROTAC EGFR degrader 6 (compound 2) (0.001-10 μM; 48 hours) exhibits potent EGFR degradation activity with certain concentration-dependent manner; and shows DC50 of 45.2 nM in HCC827 cells[1].
PROTAC EGFR degrader 6 (100 nM; 4-96 hours) degradates EGFR protein in a time-dependent manner, and reaches the maximum degradation rate (Dmax = 87%) at 96 h[1].
PROTAC EGFR degrader 6 (0.1, 1 and 10 μM; 48 hours) shows weak degradation activity on EGFR in H1975 and A549 cells[1].
PROTAC EGFR degrader 6 (0.1 and 1 μM; 32 hours) induce HCC827 apoptosis, and the percentages of apoptosis cells are 53.72% and 32.31% at 0.1 and 1 μM, respectively[1].

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

Molecular Weight

913.05

Formula

C49H57FN12O5

CAS No.
SMILES

O=C1CCC(C(N1)=O)N2CC3=C(C2=O)C=CC=C3NC(CCCCCCCN4CCN(CC4)C5=CC=C(N=C5)NC6=NC=C7N=C(N=C(C7=C6)N8CCC(CC8)CO)NC9=CC=C(C=C9)F)=O

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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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    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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PROTAC EGFR degrader 6
Cat. No.:
HY-146423
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