BLU-9931
货号：
18405-25mg 基本售价：
8190.0 元 规格：
25 mg
产品信息
概述| 货号 | 18405-25mg |
| 描述 | Fibroblast growth factor receptor 4 (FGFR4) is the receptor for fibroblast growth factor 19 (FGF19), which is a tightly controlled hormone that regulates bile acid synthesis and hepatocyte proliferation in the normal liver. Aberrant signaling through the FGFR4/FGF19 signaling complex has been implicated in hepatocellular carcinoma (HCC).1 BLU9931 is a small molecule inhibitor of FGFR4 (IC50 = 3 nM) that is selective for FGFR4 over other FGFR family members (IC50s = 591, 493, and 150 nM for FGFR1, 2, and 3, respectively) and an extensive panel of additional kinases (selectivity score for BLU9931 at 3 µM is 0.005).1 It inhibits proliferation of HCC cell lines with an activated FGFR4 signaling pathway (EC50s = 0.02-0.11 µM) and demonstrates antitumor activity when administered orally at 100 mg/kg to mice bearing HCC xenografts that overexpresses FGF19 due to amplification or to mice bearing liver tumor xenografts that overexpresses FGF19 mRNA but lack FGF19 amplification.1 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Hagel, M.,Miduturu, C.,Sheets, M., et al. First selective small molecule inhibitor of FGFR4 for the treatment of hepatocellular carcinomas with an activated FGFR4 signaling pathway. Cancer Discov. 5(4), 424-437 (2015).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 509.4 |
| 分子式 | C26H22Cl2N4O3 |
| CAS号 | 1538604-68-0 |
| 稳定性 | ≥ 2 years |
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