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Osimertinib
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Osimertinib
CAS No. : 1421373-65-0
MCE 站:Osimertinib
产品活性:Osimertinib (AZD-9291) 是一种不可逆和突变的选择性的 EGFR 抑制剂,抑制EGFRL858R 和EGFRL858R/T790M 的 IC50 分别为12 和 1 nM。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点:EGFR
In Vitro: Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC50 values ranging from 13 to 54 nM for AZD-9291. Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50 potency less than 15 nM.
In Vivo: The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day.
相关产品:Covalent Screening Library Plus | Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | FDA-Approved Drug Library | Anti-Cancer Compound Library | Drug Repurposing Compound Library | Covalent Screening Library | Differentiation Inducing Compound Library | Diabetes Related Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Anti-Hepatitis C Virus Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Targeted Therapy Drug 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
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热门标签:AZD-9291