LY2874455
作者：齐岳
发布时间：2023-08-23
09:38:08
点击数：
产品名称：LY2874455
产品描述：
| 产品描述 | LY2874455 has been used in trials studying the treatment of Advanced Cancer. |
| 靶点活性 | FGFR4:6 nM, FGFR3:6.4 nM, FGFR1:2.8 nM, FGFR2:2.6 nM, VEGFR2:7 nM |
| 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。 |
| 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. |
| 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) |
| 别名 | LY-2874455, LY 2874455 |
| 分子量 | 444.32 |
| 分子式 | C21H19Cl2N5O2 |
| CAS No. | 1254473-64-7 |
存储
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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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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