PROTAC EGFR degrader 5
PROTAC EGFR degrader 5 is 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.
(Pink: EGFR Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2409793-36-6
- Formula: C57H72FN13O5S
- Molecular Weight:1070.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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EGFR 34.8 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
>10 μM
Compound: 10
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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
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[PMID: 31951960] |
| A549 | IC50 |
>10 μM
Compound: 10
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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
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[PMID: 31951960] |
| HCC827 | IC50 |
0.22 μM
Compound: 10
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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
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[PMID: 31951960] |
| NCI-H1975 | IC50 |
>10 μM
Compound: 10
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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
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[PMID: 31951960] |
In Vitro
PROTAC EGFR degrader 5 (compound 10, 0.1-10 μM; 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.
Chemical Information
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CAS No. 2409793-36-6
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Molecular Weight 1070.33
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Formula C57H72FN13O5S
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC EGFR degrader 5 Related Classifications
HY-146422 Related Classifications
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