| 名稱 | LY2874455 |
| 描述 | LY2874455 has been used in trials studying the treatment of Advanced Cancer. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在攜帶RT-112,OPM-2（DSMZ）,SNU-16或NCI-H460異種移植物的小鼠中,LY2874455（3 mg/kg,口服）導(dǎo)致腫瘤生長的劑量依賴性抑制.LY2874455在小鼠心臟組織中,表現(xiàn)出對FGF誘導(dǎo)的Erk磷酸化的有效抑制,TED50和TED90值分別為1.3 和 3.2 mg/kg. |
| 體內(nèi)活性 | LY2874455在KMS-11,OPM-2,SNU-16和KATO-III細(xì)胞中顯示FGFR依賴性抗增殖作用。在RT-112細(xì)胞,HUVECs,KATO-III細(xì)胞和SNU-16細(xì)胞中,LY2874455抑制FGF/FGFR介導(dǎo)的信號傳導(dǎo)活性。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 82 mg/mL (184.6 mM)
Ethanol : 53 mg/mL (119.3 mM)
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| 關(guān)鍵字 | Fibroblast growth factor receptor | inhibit | FGFR | Inhibitor | LY2874455 |
| 相關(guān)產(chǎn)品 | Amlexanox | Ribociclib | Formononetin | Axitinib | Sorafenib tosylate | Lenvatinib mesylate | Ferulic Acid | Regorafenib | Pazopanib | Nintedanib | Sorafenib | Regorafenib monohydrate |
| 相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 抗癌活性化合物庫 | 已知活性化合物庫 | 激酶抑制劑庫 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | 酪氨酸激酶分子庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |