| 名称 | LY2874455 |
| 描述 | LY2874455 has been used in trials studying the treatment of Advanced Cancer. |
| 细胞实验 | Cells (2,000 per well) are first grown in RPMI for 6 hours and treated with LY2874455 at 37 ℃ for 3 days. The cells are stained at 37℃ for 4 hours and then solubilized at 37℃ for 1 hour. Finally, the plate is read at 570 nm using a plate reader (Spectra Max Gemini XS). (Only for Reference) |
| 激酶实验 | Biochemical filter-binding assays for detection of FGFR phosphorylation activities : Reaction mixtures contains 8 mM Tris-HCl (pH 7.5), 10 mmol/L HEPES, 5 mM dithiothreitol, 10 μM ATP, 0.5 μCi 33P-ATP, 10 mM MnCl2, 150 mM NaCl, 0.01% Triton X-100, 4% dimethyl sulfoxide, 0.05 mg/mL poly(Glu:Tyr) (4:1, average molecular weight of 20–50 kDa), and 7.5, 7.5, and 16 ng of FGFR1, FGFR3, and FGFR4, respectively, and are incubated at room temperature for 30 minutes followed by termination with 10% H3PO4. The reaction mixtures are transferred to 96-well MAFB filter plates that are washed 3 times with 0.5% H3PO4. After air-drying, the plates are read with a Trilux reader. |
| 体外活性 | 在携带RT-112,OPM-2（DSMZ）,SNU-16或NCI-H460异种移植物的小鼠中,LY2874455（3 mg/kg,口服）导致肿瘤生长的剂量依赖性抑制.LY2874455在小鼠心脏组织中,表现出对FGF诱导的Erk磷酸化的有效抑制,TED50和TED90值分别为1.3 和 3.2 mg/kg. |
| 体内活性 | LY2874455在KMS-11,OPM-2,SNU-16和KATO-III细胞中显示FGFR依赖性抗增殖作用。在RT-112细胞,HUVECs,KATO-III细胞和SNU-16细胞中,LY2874455抑制FGF/FGFR介导的信号传导活性。 |
| 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 | DMSO : 82 mg/mL (184.56 mM), Sonication is recommended.
Ethanol : 53 mg/mL (119.29 mM), Sonication is recommended.
|
| 关键字 | VEGFR2 | LY2874455 | Inhibitor | inhibit | Fibroblast growth factor receptor | FGFR4 | FGFR3 | FGFR2 | FGFR1 | FGFR |
| 相关产品 | Amlexanox | Ribociclib | Formononetin | Axitinib | Sorafenib tosylate | Lenvatinib mesylate | Ferulic Acid | Regorafenib | Pazopanib | Nintedanib | Sorafenib | Regorafenib monohydrate |
| 相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 抗癌化合物库 | 已知活性化合物库 | 抗结直肠癌化合物库 | 激酶抑制剂库 | 膜蛋白靶向化合物库 | 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 |