Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ASP5878 是一种 FGFR 1 (IC50:0.47 nM)、FGFR 2 (IC50:0.6 nM)、FGFR 3 (IC50:0.74 nM)、和 FGFR 4 (IC50:3.5 nM)的抑制剂,具有口服活性,具有潜在的抗肿瘤作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 678 | 现货 | ||
2 mg | ¥ 980 | 现货 | ||
5 mg | ¥ 1,930 | 现货 | ||
10 mg | ¥ 2,950 | 现货 | ||
25 mg | ¥ 4,880 | 现货 | ||
50 mg | ¥ 6,770 | 现货 | ||
100 mg | ¥ 9,130 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,130 | 现货 |
产品描述 | ASP5878 potently inhibited the tyrosine kinase activities of recombinant FGFR1, 2, 3, and 4 with IC50 values of 0.47, 0.60, 0.74, and 3.5 nmol/L. |
靶点活性 | FGFR4:3.5nM, FGFR3:0.74nM, FGFR1:0.47nM, FGFR2:0.6nM |
体内活性 | sorafenib administration for 14 days caused 40% tumor growth inhibition in the Hep3B2.1-7 xenograft model. Even after continuous sorafenib treatment, the Hep3B2.1-7 tumor gradually enlarged, and 47% tumor growth inhibition was observed by day 31. In contrast, the switch from sorafenib to ASP5878 on day 14 induced 83% tumor regression on day 52 relative to the tumor size observed on day 14. This indicates the therapeutic potential of ASP5878 for FGF19-overexpressing HCC patients who previously received sorafenib treatment. |
激酶实验 | Inhibitory activities of 128 serine/threonine kinases were measured using the Mobility Shift Assay Kit.?IC50 values were determined for kinases that were inhibited by more than 50% by 200 nmol/L of ASP5878. |
细胞实验 | The human HCC cell lines,?The experiments were conducted using low-passage cultures of these stocks.?The cells were seeded in 96-well plates and incubated overnight.?The cells were treated with ASP5878 for 5 days.?Cell viability was measured using CellTiter-Glo. |
动物实验 | HuH-7-Luc cells were inoculated into hepatic parenchyma at 3×10^5 cells/0.01 mL (Matrigel 100%)/mouse.?One week after inoculation, the mice were divided into three groups (n = 5 per group) on day 0 on the basis of bioluminescent imaging.?Vehicle (Cremophor EL/ethanol or 0.5% MC), sorafenib (30 mg/kg), or ASP5878 (3 mg/kg) was administered as a once-daily oral dose for 91 days.?Tumor growth was monitored by in vivo bioluminescent imaging of the abdomen after intraperitoneally injecting luciferin using IVIS-Lumina2.?During the study period (181 days), the survival of mice bearing hepatic tumors was recorded.?The condition of the mice was monitored daily.?The mice were scored as dead if any of the following signs of suffering were observed: cachexia, weakening, and difficulty in moving or eating.?Mice that were scored as dead were euthanized. |
别名 | ASP-5878 |
分子量 | 407.37 |
分子式 | C18H19F2N5O4 |
CAS No. | 1453208-66-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (613.69 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4548 mL | 12.2739 mL | 24.5477 mL | 61.3693 mL |
5 mM | 0.491 mL | 2.4548 mL | 4.9095 mL | 12.2739 mL | |
10 mM | 0.2455 mL | 1.2274 mL | 2.4548 mL | 6.1369 mL | |
20 mM | 0.1227 mL | 0.6137 mL | 1.2274 mL | 3.0685 mL | |
50 mM | 0.0491 mL | 0.2455 mL | 0.491 mL | 1.2274 mL | |
100 mM | 0.0245 mL | 0.1227 mL | 0.2455 mL | 0.6137 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。
ASP5878 1453208-66-6 Angiogenesis Tyrosine Kinase/Adaptors FGFR ASP-5878 Inhibitor ASP 5878 Fibroblast growth factor receptor inhibit inhibitor