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JBJ-04-125-02

  Cat. No.:  DC28949   Featured
Chemical Structure
2140807-05-0
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2140807-05-0
SMILES: O=C(NC1=NC=CS1)C(C2=CC(F)=CC=C2O)N(CC3=C4C=C(C5=CC=C(N6CCNCC6)C=C5)C=C3)C4=O
Formula: C29H26FN5O3S
M.Wt: 543.61
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. To C, et al. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 Jul;9(7):926-943.
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].
Target: EGFR (L858R/T790M):0.26 nM (IC50)
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.
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.
References: [1]. To C, et al. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 Jul;9(7):926-943.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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