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ASP5878

ASP5878

产品编号 T5473   CAS 1453208-66-6
别名: ASP-5878

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。

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ASP5878 Chemical Structure
ASP5878, CAS 1453208-66-6
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
其他形式的 ASP5878:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: ASP5878 (T5473)
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纯度: 99.86%
纯度: 99.8%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 250 mg/mL (613.69 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Futami T, et al. ASP5878, a Novel Inhibitor of FGFR1, 2, 3, and 4, Inhibits the Growth of FGF19-Expressing Hepatocellular Carcinoma. Mol Cancer Ther. 2017 Jan;16(1):68-75.
Infigratinib phosphate FGFR1 inhibitor-10 KI8751 ZM323881 hydrochloride Amlexanox FGFR4-IN-4 Dovitinib Dilactic Acid Fisogatinib

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 膜蛋白靶向化合物库 激酶抑制剂库 酪氨酸激酶分子库 抑制剂库 抗癌活性化合物库 药物功能重定位化合物库 抗癌药物库 成骨分子库 抗乳腺癌化合物库

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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。

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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。

Keywords

ASP5878 1453208-66-6 Angiogenesis Tyrosine Kinase/Adaptors FGFR ASP-5878 Inhibitor ASP 5878 Fibroblast growth factor receptor inhibit inhibitor

 

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