1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Mutated EGFR-IN-3

Mutated EGFR-IN-3 

Cat. No.: HY-130608
Handling Instructions

Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.

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

Mutated EGFR-IN-3 Chemical Structure

Mutated EGFR-IN-3 Chemical Structure

CAS No. : 2375107-27-8

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively[1].

IC50 & Target[1]

EGFRL858R/T790M

12 nM (IC50)

EGFRC797S

13 nM (IC50)

In Vitro

Mutated EGFR-IN-3 inhibits EGFR through an allosteric mechanism, biochemical IC50 values at varying ATP concentrations: 10 µM, 10.0 µM, 100.0 µM, 1000.0 µM are 15 nM, 8.3nM,11.0 nM and 8.3 nM, respectively for L858R/T790M cells[1].
Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 7.0 µM, 3.3 µM, 3.8 µM, 4.0 µM and 4.5 µM for parental, WT, L858R, L858R/T790M and L858R/T790M/C797S, respectively in the absence of Cetuximab in Ba/F3 cells[1].
Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 3.2 µM, 2.7 µM, 0.36 µM and 0.20 µM for WT,L858R, L858R/T790M and L858R/T790M/C797S, respectively in the presence of Cetuximab in Ba/F3 cells[1].

Molecular Weight

508.59

Formula

C₃₁H₂₉FN₄O₂

CAS No.

2375107-27-8

SMILES

O=C1C2=CC(OC3=CC=C(N4CCN(C)CC4)C=C3)=CC=C2NC5=CC=C(F)C=C5N1CC6=CC=CC=C6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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.
  • 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

Keywords:

Mutated EGFR-IN-3EGFREpidermal growth factor receptorErbB-1HER1TKIBa/F3cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Mutated EGFR-IN-3
Cat. No.:
HY-130608
Quantity:
MCE Japan Authorized Agent: