1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR
  3. JBJ-09-063

JBJ-09-063 

Cat. No.: HY-147183
Handling Instructions

JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer.

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

JBJ-09-063 Chemical Structure

JBJ-09-063 Chemical Structure

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Description

JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer[1].

IC50 & Target[1]

EGFR L858R

0.147 nM (IC50)

EGFR L858R/T790M

0.063 nM (IC50)

EGFR L858R/T790M/C797S

0.083 nM (IC50)

EGFRLT/L747S

0.396 nM (IC50)

In Vitro

JBJ-09-063 is remarkably effective at inhibiting cell growth and leads to a significant increase in apoptosis, even though H3255GR cells are resistant to gefitinib as a single agent, as they contain an EGFR T790M mutation[1].
JBJ-09-063 is effective in H1975 cells exogenously expressing the Osimertinib-resistant mutations[1].

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

Molecular Weight

556.65

Formula

C31H29FN4O3S

SMILES

O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(C6CCN(C)CC6)C=C5)C=C3)C4=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
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Product Name:
JBJ-09-063
Cat. No.:
HY-147183
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