JBJ-04-125-02

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

JBJ-04-125-02 

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/T790M 的 IC50 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。

JBJ-04-125-02

JBJ-04-125-02 Chemical Structure

CAS No. : 2060610-53-7

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生物活性

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].

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/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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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/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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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.
参考文献

  • [1]. To C, et al. Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 2019 Jul;9(7):926-943.

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