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。

AZ-5104

CAS No. : 1421373-98-9

MCE 站：AZ-5104

产品活性：AZ-5104是AZD 9291的活性，去甲基化代谢物。AZ-5104是 EGFR 抑制剂；抑制EGFR^L858R/T790M，EGFR^L858R，EGFR^L861Q，EGFR 和ErbB4的 IC₅₀ 值分别为1，6，1，25和7 nM。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: AZ-5104 inhibits EGFR phosphorylation with IC₅₀s of 2, 1, 2, 53, and 33 nM in H1975 (EGFR^L858R/T790M), PC-9VanR (EGFR^{Exon 19 deletion/T790M}), PC-9 (EGFR^{Exon 19 deletion}), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity.

In Vivo: The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Covalent Screening Library  |  Differentiation Inducing Compound Library  |  Anti-Hepatitis C Virus Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Gefitinib  |  Trastuzumab  |  Erlotinib  |  Cetuximab  |  AG490  |  Genistein  |  AG-1478  |  Pertuzumab  |  BI-4020  |  NSC 228155  |  Pelitinib  |  Mubritinib  |  TX1-85-1  |  Canertinib  |  Butein  |  PD168393  |  Daphnetin  |  EGFR-IN-7  |  AEE788  |  Chrysophanol  |  PD153035  |  Tyrphostin 23  |  Lavendustin A  |  Trastuzumab emtansine  |  BMS-599626 Hydrochloride  |  PD158780  |  AV-412

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。