2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage Apoptosis
  3. EGFR Akt PERK Apoptosis
  4. EGFR-IN-181

EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases.

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

EGFR-IN-181

EGFR-IN-181 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.

EGFR-IN-181 Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

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

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases[1].

IC50 & Target

Akt

 

EGFR (C797S/T790M/L858R)

 

In Vitro

EGFR-IN-181 (Compound D18) (0.001-1000 μg/mL, 48 h) shows significant anti-proliferative activity against various EGFR mutant cell lines and has a high IC50 against normal cells (MCR-5, HEK293, LX-2)[1].
EGFR-IN-181 (50-500 nM, 24 h) concentration-dependently inhibits EGFR phosphorylation (p-EGFR) and its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK) in NCI-H1975 cells (carrying EGFRL858R/T790M/C797S)[1].
EGFR-IN-181 (50-500 nM, 24 h) concentration-dependently induces apoptosis in NCI-H1975 EGFRL858R/T790M/C797S cells and causes G2 phase arrest[1].
EGFR-IN-181 inhibits hERG potassium channels in HEK293 cells with an IC50 of 10.55 μM[1].

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

EGFR-IN-181 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A549 cell line: harboring EGFRWT BaF3™ cell line: engineered BaF3 cell line, harboring EGFRL858R/T790M/C797S NCI–H1975 cell line: harboring EGFRL858R/T790M/C797S PC-9 cell line: harboring EGFRDel19 H1975 cell line: harboring EGFRL858R/T790M MCR-5, HEK293, LX-2
Concentration: 0.001 μg/mL, 0.01 μg/mL, 0.1 μg/mL, 1 μg/mL, 10 μg/mL, 100 μg/mL, 1000 μg/mL
Incubation Time: 48 h
Result: A549 (IC50 = 2.63 μM)
PC-9 (IC50 = 0.012 μM)
H1975 (IC50 = 0.027 μM)
BaF3TM (IC50 = 0.049 μM)
NCI–H1975 (IC50 = 0.87 μM)
MCR-5 (IC50 = 4.51 μM)
HEK293 (IC50 = 36.17 μM)
LX-2 (IC50 = 4.84 μM)

Western Blot Analysis[1]

Cell Line: NCI-H1975 EGFRL858R/T790M/C797S
Concentration: 50 nM, 100 nM, 500 nM
Incubation Time: 24 h
Result: Concentration-dependently inhibited EGFR phosphorylation (p-EGFR) and its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK) in NCI-H1975 cells EGFRL858R/T790M/C797S; at a concentration of 500 nM, EGFR phosphorylation was completely inhibited.

Apoptosis Analysis[1]

Cell Line: NCI-H1975 EGFRL858R/T790M/C797S cells
Concentration: 50 nM, 150 nM, 250 nM, 500 nM
Incubation Time: 24 h
Result: Induced apoptosis in a degree-dependent manner, achieving an apoptosis rate of 37.94% at a concentration of 500 nM.

Cell Cycle Analysis[1]

Cell Line: NCI-H1975 EGFRL858R/T790M/C797S cells
Concentration: 50 nM, 150 nM, 250 nM, 500 nM
Incubation Time: 24 h
Result: Induced G2 phase arrest in a concentration-dependent manner, with the proportion of cells in G2 phase being 22.57 % at 50 nM and increasing to 65.98 % at 500 nM.
In Vivo

EGFR-IN-181 (Compound D18) (12.5-25 mg/kg, p.o., once daily for 15 days ) significantly inhibits the growth of EGFR-mutant tumors in NCI-H1975 cells EGFRL858R/T790M/C797S xenograft mice in a dose-dependent manner, demonstrating good safety and tolerability with no significant toxicity[1].

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

Animal Model: A xenograft tumor model was established using female BALB/c nude mice (6-8 weeks old) by subcutaneous transplantation of NCI-H1975 cells EGFRL858R/T790M/C797S triple mutations)[1].
Dosage: 12.5 mg/kg, 25 mg/kg
Administration: P.o., once daily for 15 days
Result: At a dose of 12.5 mg/kg, the tumor growth inhibition rate (TGI) was 53.64 %; at a dose of 25 mg/kg, the TGI was 91.04 %.
The average tumor weight was significantly lower than that of the control group.
Did not experience a significant decrease in body weight, and H&E staining of the major organs (heart, liver, spleen, lung, and kidney) showed no lesions or organ failure.
Molecular Weight

482.95

Formula

C24H28ClN6OP
SMILES

CP(C)(C1=CC=CC=C1NC2=NC(NC3=CC4=C(N(CCN(C)C)C=C4)C=C3)=NC=C2Cl)=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.

EGFR-IN-181 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:

EGFR-IN-181EGFRAktPERKApoptosisEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseNSCLCNon-Small Cell Lung CancerBlood-brain barrierInhibitorinhibitorinhibit

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:
EGFR-IN-181
Cat. No.:
HY-178939
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.