| 名称 | SGX-523 |
| 描述 | SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf. |
| 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
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : 1.37 mg/mL (3.81 mM), Suspension.
DMSO : 13.7 mg/mL (38.12 mM), Sonication is recommended.
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| 关键字 | SGX-523 | SGX523 | SGX 523 | selective | p38α | p38MAPK | p38 MAPK | MET | Inhibitor | inhibit | HGFR | exquisitely | C-Raf | c-Met/HGFR | cMet/HGFR | c-Met | cMet | B-Raf (V599E) | BcrAbl | antitumor | Abl |
| 相关产品 | D-Psicose | Afatinib | Dabrafenib | Undecane | Dasatinib | (Rac)-Hesperetin | Sorafenib | Decanoic Acid | Fumaric acid | Bisphenol A | Esculin | Bacitracin Zinc |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 激酶抑制剂库 | 抗衰老化合物库 | 免疫/炎症分子化合物库 | 疼痛相关化合物库 | 酪氨酸激酶分子库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |