JBJ-04-125-02

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JBJ-04-125-02 是一种有效的突变选择性、变构和口服活性 EGFR 抑制剂，对 EGFRL858R/T790M 的 IC50 为 0.26 nM。 JBJ-04-125-02可以抑制癌细胞增殖和EGFRL858R/T790M/C797S信号传导。 JBJ-04-125-02具有抗肿瘤活性。

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.

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.

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 weeksResult:Led to marked tumor regressions within 4 weeks of treatment.

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Angiogenesis

EGFR

EGFR (L858R/T790M)

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2060610-53-7

543.61

C??H??FN?O?S

>98% (HPLC)

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(-20℃)

With Ice Pack

≥ 2 years