MCE 的所有產品僅用作科學研究或藥證申報，我們不為任何個人用途提供產品和服務。

AZD4547

產品活性：AZD4547 (ADSK091) 是一種有效的 FGFR 家族抑制劑，作用于 FGFR1，FGFR2，FGFR3 和 FGFR4，IC₅₀ 分別為 0.2 nM，2.5 nM，1.8 nM 和 165 nM。

研究領域：Protein Tyrosine Kinase/RTK

作用靶點：FGFR

In Vitro: AZD4547 also inhibits recombinant VEGFR2 (KDR) kinase activity with an IC₅₀ of 24 nM. In KG1a, Sum52-PE, MCF7, and KMS11 cell lines, AZD4547 potently inhibits autophosphorylation of FGFR1, 2, and 3 tyrosine kinases (IC₅₀ values of 12, 2, and 40 nM, respectively) and displays weaker inhibition of FGFR4 cellular kinase activity (IC₅₀=142 nM). Significantly weaker inhibitory activity is observed versus cellular KDR and IGFR ligand-induced phosphorylation (IC₅₀ values of 258 and 828 nM, respectively), representing approximately 20- and 70-fold selectivity over cellular FGFR1. Besides, AZD4547 potently inhibits FGFR phosphorylation and downstream signaling affected through FRS2, PLCγ, and MAPK at the cellular level.

In Vivo: Female SCID mice bearing KMS11 tumors are randomized and treated chronically with AZD4547 at a range of well-tolerated doses. Oral AZD4547 treatment results in dose-dependent tumor growth inhibition. Twice daily administration of AZD4547 at 3 mg/kg gives statistically significant tumor growth inhibition of 53% (P<0.0005 by one-tailed t test) when compare with vehicle-treated controls, whereas doses of 12.5 mg/kg once daily and 6.25 mg/kg twice daily results in complete tumor stasis (P<0.0001). A further efficacy study in the KG1a model with 12.5 mg/kg once daily AZD4547 results in 65% tumor growth inhibition (P=0.002).

相關產品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Reprogramming Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Angiogenesis-Related Compound Library  |  Targeted Diversity Library  |  Anti-Liver Cancer Compound Library   |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  FGFR4-IN-12  |  FGFR2-IN-2  |  Multi-kinase-IN-2  |  FGFR1 inhibitor-6  |  FGFR4-IN-4  |  FGFR3-IN-3  |  FGFR-IN-7  |  PP58  |  FGFR4-IN-10  |  Vosoritide acetate  |  ODM-203  |  ENMD-2076 Tartrate  |  R1530  |  Gunagratinib  |  Ponatinib hydrochloride  |  Nintedanib  |  Heparan Sulfate  |  CPL304110  |  Futibatinib  |  Trafermin  |  Roblitinib  |  PD173074  |  FGFR-IN-2  |  Lucitanib  |  Masitinib  |  Nintedanib-¹³C,d₃  |  Zoligratinib  |  BLU9931  |  MAX-40279 hemifumarate  |  Pazopanib-¹³C,d₃ (hydrochloride)

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種*僅有化合物庫，我們致力于為*科研客戶提供前沿的高品質小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動劑涉及各熱門信號通路及疾病領；
•   產品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產品，廣泛應用于新藥研發、生命科學等科研項目；
•   提供虛擬篩選，離子通道篩選，代謝組學分析檢測分析，藥物篩選等專業技術服務；
•   設有專業的實驗中心和嚴格的質控、驗證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質檢報告，確保產品的高純度、高品質；
•   產品的生物活性多經各國客戶實驗驗證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業團隊跟蹤新的制藥及生命科學研究進展，為您提供*新的活性化合物；
•   與世界各大制藥公司及*科研機構建立了長期的合作。