JBJ-02-112-05

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-02-112-05 

JBJ-02-112-05 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 15 nM。

JBJ-02-112-05

JBJ-02-112-05 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M[1].

IC50 & Target[1]

EGFRL858R/T790M

15 nM (IC50)

体外研究
(In Vitro)

In Ba/F3 cells, JBJ-02-112-05 inhibits the activities of wildtype EGFR, EGFRL858R, EGFRL858R/T790M and EGFRL858R/T790M/C797S with IC50 values of 9.29 µM; 8.35 µM; 8.53 µM and 2.13 µM, respectively[1].
JBJ-02-112-05 demonstrates mutant selectivity by inhibiting mutant EGFR and downstream AKT and ERK1/2 phosphorylation in Ba/F3 cells stably transfected with EGFRL858R, EGFRL858R/T790M, EGFRL858R/T790M/C797S mutations[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

JBJ-02-112-05 (100 mg/kg; oral gavage; once daily; for 3 days; EGFRL858R/T790M/C797S genetically engineered mice) treatment inhibits phosphorylation of EGFR and downstream signaling pathways[1].
JBJ-02-112-05 exhibits a moderate half-life of 3 hours and a Cmax of 13.7 µM following 3 mg/kg intravenous (i.v.) dose. A 5 mg/kg oral dose of JBJ-02-112-05 achieves a half-life of 16.4 hours and a CCmax of 1.31 µM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: EGFRL858R/T790M/C797S genetically engineered mice[1]
Dosage: 100 mg/kg
Administration: Oral gavage; once daily; for 3 days
Result: Inhibited phosphorylation of EGFR and downstream signaling pathways.

分子量

464.54

Formula

C27H20N4O2S
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务