1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. JBJ-02-112-05

JBJ-02-112-05 

Cat. No.: HY-135914
Handling Instructions

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M.

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

JBJ-02-112-05 Chemical Structure

JBJ-02-112-05 Chemical Structure

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Description

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M[1].

IC50 & Target[1]

EGFRL858R/T790M

15 nM (IC50)

In Vitro

In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFRL858R, EGFRL858R/T790M and EGFRL858R/T790M/C797S with IC50 values of 9.29 µM; 8.35 µM; 8.53 µM and 2.13 µM, respectively[1].
JBJ-02-112-05 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797S mutations[1].

In Vivo

JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFRL858R/T790M/C797S genetically engineered mice) treatment inhibits phosphorylation of EGFR and downstream signaling pathways[1].
JBJ-02-112-05 exhibits a moderate half-life of 3 hours and a Cmax of 13.7 µM following 3 mg/kg intravenous (i.v.) dose. A 5 mg/kg oral dose of JBJ-02-112-05 achieves a half-life of 16.4 hours and a CCmax of 1.31 µM[1].

Animal Model: EGFRL858R/T790M/C797S genetically engineered mice[1]
Dosage: 100 mg/kg
Administration: Oral gavage; once daily; for 3 days
Result: Inhibited phosphorylation of EGFR and downstream signaling pathways.
Molecular Weight

464.54

Formula

C₂₇H₂₀N₄O₂S

SMILES

O=C(NC1=NC=CS1)C(N2C(C(C=C(C3=CC(C=CN4)=C4C=C3)C=C5)=C5C2)=O)C6=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.

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Keywords:

JBJ-02-112-05EGFREpidermal growth factor receptorErbB-1HER15-indoleisoindolinoneEGFRL858R/T790Mmutant-selectiveAKTERK1/2phosphorylationInhibitorinhibitorinhibit

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Product Name:
JBJ-02-112-05
Cat. No.:
HY-135914
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