2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. PROTACs EGFR Apoptosis
  4. 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.

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

PROTAC EGFR degrader 5 Chemical Structure

PROTAC EGFR degrader 5 Chemical Structure

CAS No. : 2409793-36-6

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PROTAC EGFR degrader 5 Related Antibodies

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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)

Cellular Effect
Cell Line Type Value Description References
A-431 IC50
> 10 μM
Compound: 10
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: 10
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
0.22 μM
Compound: 10
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: 10
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 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.

PROTAC EGFR degrader 5 Related Antibodies

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 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 EGFR degrader 52409793-36-6PROTAC EGFR degrader5PROTAC EGFR degrader-5PROTACsEGFRApoptosisEpidermal growth factor receptorErbB-1HER1EGFR-TKEGFR-TK degradersProteolysis targeting chimeraPROTAC strategyInhibitorinhibitorinhibit

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