LY2874455
作者：齊岳
發布時間：2023-08-23
09:38:08
點擊數：
產品名稱：LY2874455
產品描述：
| 產品描述 | LY2874455 has been used in trials studying the treatment of Advanced Cancer. |
| 靶點活性 | FGFR4:6 nM, FGFR3:6.4 nM, FGFR1:2.8 nM, FGFR2:2.6 nM, VEGFR2:7 nM |
| 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）導致腫瘤生長的劑量依賴性抑制.LY2874455在小鼠心臟組織中,表現出對FGF誘導的Erk磷酸化的有效抑制,TED50和TED90值分別為1.3 和 3.2 mg/kg. |
| 體內活性 | LY2874455在KMS-11,OPM-2,SNU-16和KATO-III細胞中顯示FGFR依賴性抗增殖作用。在RT-112細胞,HUVECs,KATO-III細胞和SNU-16細胞中,LY2874455抑制FGF/FGFR介導的信號傳導活性。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 別名 | LY-2874455, LY 2874455 |
| 分子量 | 444.32 |
| 分子式 | C21H19Cl2N5O2 |
| CAS No. | 1254473-64-7 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 82 mg/mL (184.6 mM)
Ethanol: 53 mg/mL (119.3 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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