1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. JBJ-04-125-02

JBJ-04-125-02 

Cat. No.: HY-135805
Handling Instructions

JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.

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

JBJ-04-125-02 Chemical Structure

JBJ-04-125-02 Chemical Structure

CAS No. : 2060610-53-7

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Description

JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities[1].

IC50 & Target[1]

EGFR (L858R/T790M)

0.26 nM (IC50)

In Vitro

JBJ-04-125-02 (0-1000 nM; 72 hours; H1975 cells) treatment could inhibit cell proliferation of H1975 cells at low nanomolar concentrations[1].
JBJ-04-125-02 treatment also inhibits cell proliferation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, or EGFRL858R/T790M/C797S mutations[1].
The ability of JBJ-04-125-02 (0.01-10 μM) to inhibit EGFR phosphorylation using Ba/F3, H1975 and NIH-3T3 cells is examined. JBJ-04-125-02 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation[1].

Cell Proliferation Assay[1]

Cell Line: H1975 cells
Concentration: 0 nM, 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 72 hours
Result: Inhibited cell proliferation of H1975 cells at low nanomolar concentrations.
In Vivo

JBJ-04-125-02 (50 mg/kg; oral gavage; once daily; for 15 weeks; EGFRL858R/T790M/C797S genetically engineered mice) treatment leads to marked tumor regressions within 4 weeks of treatment[1].
JBJ-04-125-02 exhibits a moderate half-life of 3 hours and a high area under curve of 728,577 min•ng/mL (AUClast) following 3 mg/kg intravenous (i.v.) dose. A 20 mg/kg oral dose of JBJ-04-125-02 achieves an average maximal plasma concentration of 1.1 μmol/L with an oral bioavailability of 3%[1].

Animal Model: EGFRL858R/T790M/C797S genetically engineered mice (GEM)[1]
Dosage: 50 mg/kg
Administration: Oral gavage; once daily; for 15 weeks
Result: Led to marked tumor regressions within 4 weeks of treatment.
Molecular Weight

543.61

Formula

C₂₉H₂₆FN₅O₃S

CAS No.

2060610-53-7

SMILES

O=C(NC1=NC=CS1)[[email protected]@H](C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(N6CCNCC6)C=C5)C=C3)C4=O

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Room temperature in continental US; may vary elsewhere.

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

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Keywords:

JBJ-04-125-02EGFREpidermal growth factor receptorErbB-1HER1Allostericanti-proliferationT790M-mutantkinomeAKTERK1/2phosphorylationanti-tumorsingle-agentInhibitorinhibitorinhibit

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JBJ-04-125-02
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