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JBJ-04-125-02
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JBJ-04-125-02图片
CAS NO:2060610-53-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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EGFRL858R/T790MIC50为 0.26 nM。JBJ-04-125-02 可抑制癌细胞增殖和EGFRL858R/T790M/C797S信号传导。JBJ-04-125-02 具有抗肿瘤活性。
生物活性

JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally activeEGFRinhibitor with anIC50of 0.26 nM forEGFRL858R/T790M. JBJ-04-125-02 can inhibitcancercell proliferation andEGFRL858R/T790M/C797Ssignaling. JBJ-04-125-02 has anti-tumor activities[1].

IC50& Target

EGFR (L858R/T790M)

0.26 nM (IC50)

体外研究
(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/C797Smutations[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.
体内研究
(In Vivo)

JBJ-04-125-02 (50 mg/kg; oral gavage; once daily; for 15 weeks; EGFRL858R/T790M/C797Sgenetically 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 minong/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/C797Sgenetically 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.
分子量

543.61

Formula

C29H26FN5O3S

CAS 号

2060610-53-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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