JBJ-04-125-02

SKU: orb1220170

Description

JBJ-04-125-02 (0-1000 nM; 72 hours; H1975 cells) treatment could inhibit cell proliferation of H1975 cells at low nanomolar concentrations.JBJ-04-125-02 treatment also inhibits cell proliferation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, or EGFRL858R/T790M/C797S mutations.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.

Key Properties

• CAS Number: 2060610-53-7
• MW: 543.61
• Purity: >98% (HPLC)
• Formula: C??H??FN?O?S
• SMILES: O=C(NC1=NC=CS1)[C@@H](C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(N6CCNCC6)C=C5)C=C3)C4=O
• Target: EGFR

Bioactivity

• 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. 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%. Animal model: EGFRL858R/T790M/C797S genetically engineered mice (GEM). Dosage: 50 mg/kg. Administration: Oral gavage; once daily; for 15 weeks. Result: Led to marked tumor regressions within 4 weeks of treatment.
• 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. JBJ-04-125-02 treatment also inhibits cell proliferation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, or EGFRL858R/T790M/C797S mutations. 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. Cell Proliferation Assay 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

EGFR