PROTAC EGFR degrader 19
PROTAC EGFR degrader 19 is a potent EGFR PROTAC degrader. PROTAC EGFR degrader 19 bridges EGFR and VHL E3 ligase, thereby promoting ubiquitination and degradation of EGFR, which in turn blocks oncogenic signaling pathways. PROTAC EGFR degrader 19 can be used for research on non-small cell lung cancer.
(Pink: EGFR ligand (HY-189361); Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3017179-52-8
- Formula: C57H65N11O6S2
- Molecular Weight:1064.33
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
EGFR (WT) |
EGFR (ex19del/T790M) |
VHL |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1299 | IC50 |
30.45 μM
|
Inhibition of cell viability in human H1299 cells assessed by CCK-8 assay.
Inhibition of cell viability in human H1299 cells assessed by CCK-8 assay.
|
42092430 |
| PC-9 | IC50 |
15.49 μM
|
Inhibition of cell viability in human PC-9 cells assessed by CCK-8 assay.
Inhibition of cell viability in human PC-9 cells assessed by CCK-8 assay.
|
42092430 |
In Vitro
PROTAC EGFR degrader 19 (compound III-4) (0.1-1 μM; 24 h) potently degrades EGFRWT in H1299 cells, achieving 76% degradation at 0.1 μM, and effectively degrades EGFRDel19 in PC-9 cells, achieving 72% degradation at 0.1 μM[1].
PROTAC EGFR degrader 19 inhibits the viability of H1299 cells and PC-9 cells with IC50 values of 30.45 μM and 15.49 μM, respectively[1].
PROTAC EGFR degrader 19 (0.1-1 μM; 24 h) does not degrade EGFRL858R/T790M in H1975 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:H1299
-
Concentration:0.1, 1 μM
-
Incubation Time:24 h
-
Result:Induced approximately 76% degradation of EGFRWT at 0.1 μM.
Decreased degradative efficacy to approximately 59% at 1 μM, consistent with a hook effect.
-
Cell Line:PC-9
-
Concentration:0.1, 1 μM
-
Incubation Time:24 h
-
Result:Induced approximately 72% degradation of EGFRDel19 at 0.1 μM.
Decreased degradative efficacy to less than 20% at 1 μM, consistent with a hook effect.
-
Cell Line:H1975
-
Concentration:0.1, 1 μM
-
Incubation Time:24 h
-
Result:Showed no degradation activity against EGFRL858R/T790M.
Chemical Information
-
CAS No. 3017179-52-8
-
Molecular Weight 1064.33
-
Formula C57H65N11O6S2
-
SMILES
O=C1N(CC2=C1C=C(C=C2)C(C=C3)=CN=C3N4CCN(CC4)CC5CCN(CC(N[C@@H](C(C)(C)C)C(N6C[C@H](O)C[C@H]6C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)=O)=O)C5)C(C9=CC=CC=C9)C(NC%10=NC=CS%10)=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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC EGFR degrader 19 Related Classifications
HY-189360 Related Classifications
Powered by Bioz