SGX523 is selective inhibitor of the receptor tyrosine kinase MET. MET is implicated in development and progression of cancer. SGX523 ihibits MET autophosphorylation and signalling, as well as activates cysteine-aspartic acid protease 3 (caspase 3), an enzyme which is part of the apoptosis signalling cascade.

SGX523 is a drug which acts by blocking the function of an enzyme called MET. MET activity may be important in growth and survival of some types of cancer. This Phase I trial is studying the safety, side effects, and best dose of SGX523 when given to patients with advanced cancer, and how well it inhibits MET activity in tumors.

Here, we describe SGX523, a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold selective versus the >200-fold selectivity of other protein kinases tested in biochemical assays.

SGX-523是肝细胞生长因子受体 (Met)的一个新型的、有效的、ATP-竞争性并高度选择性抑制剂，IC50值为4 nM [1]。 SGX-523在胃癌细胞株GTL16（IC50值40 nM）和人类肺癌细胞株A549（IC50值12 nM）中抑制Met自身磷酸化 [1]。 此外，在口服填喂SGX-523的移植瘤型鼠派生的癌细胞系GTL16和人类GBM细胞系U87MG中观察到肿瘤退缩 [1]。 SGX523已表现出抑制大脑癌细胞系（包括U87、U373、DAOY和神经胶质瘤干细胞1228）中MEK、MAPK和Akt的磷酸化 …

SGX-523 is a novel, potent, ATP-competitive, and highly-selective Hepatocyte growth factor receptor (MET) inhibitor with IC50 value of 4 nM [1]. SGX523 inhibits MET autophosphorylation in gastric cancer cell line GTL16 and human lung carcinoma cell line A

2020年8月31日 · SBRx binders demonstrated superior electrode performance in terms of adhesion strength, cyclability, rate capability, and self-discharge suppression compared with PVdF binder. Among the SBRx binders, SBR low demonstrated the optimum performance in terms of cyclability and rate capability.

SGX523是ATP竞争性抑制剂，作用于低活性和非磷酸化的MET时亲和力更高（MET-KD (0P), K i = 2.7 nM）。 SGX523在纳摩尔浓度抑制MET调节的信号,细胞增殖和细胞迁移，但是对依赖其他 …

SGX 523 is a potent and selective c-MET kinase inhibitor (IC 50 = 4nM). Exhibits minimal inhibition against a panel of 213 other protein kinases (at 1 μ M). Suppresses growth of tumor xenografts derived from human glioblastoma, lung and gastric cancer cells.

2019年2月17日 · （高清正版） asme sec ii b sb-523_sb-523m-2013 星级： 5 页 (正版） asme sec ii b sb-75-2013 星级： 11 页 asme sec viii d1 b pt ub 星级： 10 页 asme sec viii d1 b pt uf 星级： 9 页 asme sec viii d1 b pt uw ...