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PROTAC EGFR degrader 4

PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy[1].

Product Specifications

CAS Number

2882845-50-1

UNSPSC

12352005

Target

Autophagy; EGFR; PROTACs

Type

Reference compound

Related Pathways

Autophagy; JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-egfr-degrader-4.html

Purity

99.70

Solubility

DMSO : 100 mg/mL (ultrasonic)

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(C=C5)NC6=NC=C7N=C(N(C7=N6)C8CCCC8)NC9=CC=CC=C9)=O)=O)O)=O

Molecular Formula

C55H70N12O4S

Molecular Weight

995.29

References & Citations

[1]Hong-Yi Zhao, Discovery of potent small molecule PROTACs targeting mutant EGFR. Eur J Med Chem. 2020 Dec 15;208:112781.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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