Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LY2874455 是pan-FGFR 抑制剂,能够抑制FGFR1 (IC50:2.8 nM),FGFR2 (IC50:2.6 nM),FGFR3 (IC50:6.4 nM),FGFR4 (IC50:6 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 366 | 现货 | ||
2 mg | ¥ 523 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,260 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 4,990 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 913 | 现货 |
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。 |
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 | 444.31 |
分子式 | C21H19Cl2N5O2 |
CAS No. | 1254473-64-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 82 mg/mL (184.6 mM)
Ethanol: 53 mg/mL (119.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.2507 mL | 11.2534 mL | 22.5068 mL | 56.267 mL |
5 mM | 0.4501 mL | 2.2507 mL | 4.5014 mL | 11.2534 mL | |
10 mM | 0.2251 mL | 1.1253 mL | 2.2507 mL | 5.6267 mL | |
20 mM | 0.1125 mL | 0.5627 mL | 1.1253 mL | 2.8134 mL | |
50 mM | 0.045 mL | 0.2251 mL | 0.4501 mL | 1.1253 mL | |
100 mM | 0.0225 mL | 0.1125 mL | 0.2251 mL | 0.5627 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LY2874455 1254473-64-7 Angiogenesis Tyrosine Kinase/Adaptors VEGFR FGFR Fibroblast growth factor receptor inhibit Inhibitor LY 2874455 LY-2874455 inhibitor