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Naquotinib mesylate
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Naquotinib mesylate
CAS No. : 1448237-05-5
MCE 站:Naquotinib mesylate
产品活性:Naquotinib mesylate (ASP8273 mesylate) 是有口服活性,不可逆的 EGFR 突变体抑制剂;对EGFR突变体和EGFR的 IC50 值分别为8-33和230 nM。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点:EGFR
In Vitro: In assays using endogenously EGFR-dependent cells, Naquotinib inhibits the growth of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M) and PC-9ER(del ex19/T790M) with IC50s of 8-33 nM. Naquotinib selectively inhibits phosphorylation of EGFR and its down-stream signal pathway, ERK and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431.In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective.
In Vivo: Oral Naquotinib treatment dose dependently induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models. Dosing schedules does not affect the efficacy of Naquotinib. In an NCI-H1975 xenograft model, complete regression of tumor is achieved after 14-days of Naquotinib treatment. Complete regression is maintained in 50% of mice more than 85 days after cessation of Naquotinib treatment.
相关产品:Covalent Screening Library Plus | Drug Repurposing Compound Library Plus | Clinical Compound 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 | Clinical Compound Library | Drug Repurposing Compound Library | Covalent Screening Library | Differentiation Inducing Compound Library | Anti-COVID-19 Compound Library | Orally Active 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
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热门标签:ASP8273 (mesylate)