MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

BLU9931

CAS No. : 1538604-68-0

MCE 站：BLU9931

产品活性：BLU9931 是一种有效的，高度选择性的，不可逆的成纤维细胞生长因子受体 4 (FGFR4) 抑制剂，其 IC₅₀ 值为 3 nM，K_d 值为 6 nM。BLU9931 具有显着的抗肿瘤活性。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR

In Vitro: BLU9931 inhibits proliferation of HCC cell lines that express an intact FGFR4 signaling complex, with EC₅₀s of 0.07 μM, 0.11 μM and 0.02 μM for Hep 3B, HuH7 and JHH7 cells, respectively.
BLU9931 (0.3-300 nM; 1 hour; MDA-MB-453 and Hep 3B cells) treatment demonstrates potent, dose-dependent reduction of phosphorylation of FGFR4 signaling pathway components, including fibroblast growth factor receptor substrate 2 (FRS2), MAPK, and AKT in MDA-MB-453 cells. BLU9931 shows dose-dependent inhibition of the signaling cascade downstream of FGFR4. BLU9931 exhibits potent inhibition of phosphorylation of the FGFR4 pathway components in Hep 3B cells. BLU9931 treatment leads to induction of caspase-3/7 activity, indicative of induction of apoptosis that results in inhibition of signaling downstream of FGFR4.
BLU9931 (100 nM; 0 -24 hours; Hep 3B cells) treatment increases CYP7A1 mRNA expression and the expression of the proliferative marker EGR1 is inhibited.

In Vivo: BLU9931 (10-100 mg/kg; oral administration; twice every day; for 21 days; mice) treatment demonstrates antitumor activity in HCC xenograft models.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Covalent Screening Library  |  Reprogramming Compound Library  |  Anti-Lung Cancer Compound Library  |  SU 5402  |  Heparan Sulfate  |  PD173074  |  Formotin  |  Gandotinib  |  KW-2449  |  Ferulic acid  |  PD-166866  |  CP-547632  |  PP58  |  SUN11602  |  R1530  |  2,5-Dihydroxybenzoic acid  |  Tyrosine kinase-IN-1  |  PD-161570  |  ARQ 069  |  PD-089828  |  SM1-71  |  SU4984

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。