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JBJ-04-125-02

CAS No. : 2060610-53-7

MCE 站：JBJ-04-125-02

产品活性：JBJ-04-125-02 是一种有效的，选择性突变，变构和口服活性的 EGFR 抑制剂，对 EGFR^L858R/T790M 的 IC₅₀ 为 0.26 nM。JBJ-04-125-02 可抑制癌细胞增殖和 EGFR^{L858R/T790M/C797S} 信号传导。JBJ-04-125-02 具有抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling

作用靶点：EGFR

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 EGFR^L858R, EGFR^L858R/T790M, or EGFR^{L858R/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.

In Vivo: JBJ-04-125-02 (50 mg/kg; oral gavage; once daily; for 15 weeks; EGFR^{L858R/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%.

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