化合物SGX-523 T2293

Product Introduction
Bioactivity


英文名: SGX-523

描述: SGX523 是选择性的和 ATP 竞争性的MET 抑制剂 (IC50:4 nM)。它对 MET 的选择性其它他蛋白激酶高 1000 倍。它具有抗肿瘤特性。

细胞实验: MDCK cells are seeded at 1 × 103 per well in a 24-well plate and incubated at 37 °C in 5% CO2 for 1 week in MEM and 10% fetal bovine serum. HGF (90 ng/mL) and various concentrations of SGX523 are added and the cells are incubated for another 18 hours (37 °C, 5% CO2 humidified incubator) and visualized. A549 cells are plated in 12-well plates (6 × 104 per well) and incubated to confluence to investigate cell migration. A channel is introduced into the monolayers by scratching with a pipette tip. Various dilutions of compound are added in starve medium in the presence and absence of HGF (90 ng/mL).The wells are checked for cell migration after twenty-fou(Only for Reference)

激酶实验: Kinase assays: Initial rate constants are measured at 21 °C in the presence of 100 mM HEPES (pH 7.5), 0.3 mg/mL poly(Glu-Tyr) peptide substrate, 10 mM MgCl2, 1 mg/mL bovine serum albumin, 5% DMSO, 20 nM MET-KD and various concentrations of ATP and SGX523. Total reaction volumes (20 μL) are quenched with 20 μL Kinase-Glo detection buffer. Luminescence is detected in a plate-reading luminometer and the results are analyzed by nonlinear regression.

体外活性: SGX523（≥10 mg/kg,2次/天,p.o.）可使预计的GTL16肿瘤生长显著延迟.SGX523（30 mg/kg,2次/天）对U87 mg肿瘤生长的抑制效果较明显,其还延迟H441肿瘤生长,且降低MET自磷酸化水平.

体内活性: 纳摩尔浓度的SGX523可抑制MET调节的信号、细胞增殖及迁移,但对依赖其他蛋白激酶（如RON）的信号无抑制作用,即使浓度达到微摩级。SGX523可抑制体内MET,这与其剂量依赖性抑制人类恶性胶质瘤、肺癌及胃癌衍生的移植瘤生长有关,表明上述肿瘤对MET的催化活性有依赖性。SGX-523是c-Met/肝细胞生长因子受体酪氨酸激酶抑制剂,可使MET失活而不能与其他蛋白激酶发生相互作用。SGX523对纯化的MET催化区具有明显的抑制效果,但对与之紧密相关的RON无作用。作为ATP竞争性抑制剂,SGX523对低活性和非磷酸化的MET（MET-KD(0P),Ki： 2.7 nM）亲和力更高。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 3.59 mg/mL (10 mM)


关键字: inhibit | c-Met/HGFR | Inhibitor | antitumor | selective | exquisitely | MET | SGX-523 | SGX523 | SGX 523

相关产品: LY3009120 | B-Raf IN 11 | Pelitinib | K-Ras(G12C) inhibitor 9 | GW 441756 | I-49 free base | TBAP-001 | I-37 | ARS-853 | Pseudoginsenoside Rh2

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Tyrosine Kinase Inhibitor Library | Highly Selective Inhibitor Library

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