2. PROTAC Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. PROTACs EGFR Apoptosis
  4. PROTAC EGFR degrader 14

PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFRC797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFRWT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)).

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

PROTAC EGFR degrader 14

PROTAC EGFR degrader 14 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PROTAC EGFR degrader 14 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFRC797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFRWT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688))[1].

In Vitro

PROTAC EGFR degrader 14 (Compound 9ea) (0-2x104 nM, 0-24 h) concentration- and dose-dependently degrades EGFR in PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells, with DC50 values of 2.9 and 21.6 nM respectively and is inactive in the EGFR wild-type cell line (A549, DC50 = 2157 nM)[1].
PROTAC EGFR degrader 14 (0.1-5 μM, 24-48 h) induces G1 phase arrest and cell apoptosis in PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells [1].
PROTAC EGFR degrader 14 (0.01-0.25 μM, 24 h) effectively reduces EGFR degradation and it depends on the proteasome and VHL system in PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells [1].

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

PROTAC EGFR degrader 14 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells
Concentration: 0.1, 0.5, 1 and 5 μM
Incubation Time: 24 h
Result: Increased the percentages of cells in the G1/G0 phase concentration-dependently.
Reduced the S phase populations 24.8% to 10.4% in PC9 (EGFRL858R/T790M/C797S) cells and 22.3% to 10.9% in PC9 (EGFRDel19/T790M/C797S) cells.

Apoptosis Analysis[1]

Cell Line: PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells
Concentration: 0.1, 0.5, 1 and 5 μM
Incubation Time: 48 h
Result: Significantly promoted cell apoptosis in a concentration-dependent manner.
Reached the apoptotic rates of 22.0% and 36.5%, respectively.

Western Blot Analysis[1]

Cell Line: PC9 (EGFRL858R/T790M/C797S) and PC9 (EGFRDel19/T790M/C797S) cells
Concentration: 0.01, 0.05, 0.25 μM
Incubation Time: 24 h
Result: Effectively inhibited downstream signaling proteins as the phosphorylation of STAT3, AKT and ERK1/2.
Showed weaker inhibition of EGFR and downstream signaling proteins in A549 cells.

Western Blot Analysis[1]

Cell Line: PC9 (EGFRL858R/T790M/C797S), PC9 (EGFRDel19/T790M/C797S) cells and A549 (EGFRWT)
Concentration: 0.25 μM pretreated with MG132 (HY-13259) (10 μM), MLN4924 (HY-70062) (10 μM), and VHL ligand (10 μM and 20 μM) for 4 h
Incubation Time: 24 h
Result: Effectively blocked EGFR degradation by pretreatment with the proteasome inhibitor MG132 or the E1 neddylation inhibitor MLN4924.
Exhibited no effect in inducing EGFR degradation without VHL ligand.
In Vivo

PROTAC EGFR degrader 14 (Compound 9ea) (25-50 mg/kg, i.v., every other day, for 15 days) significantly inhibits tumor growth in PC9 (EGFRL858R/T790M/C797S) xenografts mice model, with potent EGFR degradation efficacy and no signs of toxicity[1].

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

Animal Model: PC9 (EGFRL858R/T790M/C797S) xenografts model in male BALB/c nude mice[1]
Dosage: 25 and 50 mg/kg
Administration: Intravenous injection (i.v.), every other day, for 15 days
Result: Demonstrated superior efficacy with the tumor growth inhibition (TGI) rate of 74.7%.
No statistically significant body weight loss was observed in mice during the treatment period.
Significantly reduced the average tumor weight.
Displayed no toxicity on the primary organs, including the heart, liver, spleen, lungs, kidneys, and brain.
Caused no significant changes in blood parameters analysis and blood biochemistry profiling.
Molecular Weight

1008.33

Formula

C57H73N11O4S
SMILES

O=C(CCCCCCN1CCN(C2=CC=C(NC3=NC=C4C(N(C(CNC5=CC=CC=C5)=C4)C6CCCC6)=N3)C=C2)CC1)N[C@@H](C(C)(C)C)C(N7[C@H](C(NCC8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PROTAC EGFR degrader 14 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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 14PROTAC EGFR degrader14PROTAC EGFR degrader-14PROTACsEGFRApoptosisEpidermal growth factor receptorErbB-1HER1nonsmall cell lung cancerPROTACXenograft mouse modelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC EGFR degrader 14
Cat. No.:
HY-175252
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.