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CAS No. : 1934259-00-3
MCE 国际站:limertinib
产品活性:limertinib (ASK120067) 是一种有效的口服活性 EGFRT790M 抑制剂 (IC50:0.3 nM),对 EGFRWT(IC50:6.0 nM) 具有选择性。limertinib 是用于非小细胞肺癌 (NSCLC) 研究的第三代 EGFR-TKI。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点:EGFR
In Vitro: In the in vitro kinase assay limertinib potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of limertinib against wild-type EGFR (EGFRWT) is 6 nM.limertinib selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC50 values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFRWT), with IC50 values ranging from 338 nM to 1541 nM.limertinib (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFRL858R/T790M) even at low dosage (0.1-1 nM). Additionally, limertinib inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM.
In Vivo: limertinib (oral gavage; 5-20 mg/kg; once daily; 21 days) results in significantly regressed tumor growth, with a tumor growth inhibition (TGI) rate of 85.7%, and administration of 10 mg/kg limertinib causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib.
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 | Orally Active Compound Library | Anti-Hepatitis C Virus Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Targeted Diversity Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | EGFR/HER2/CDK9-IN-2 | Lapatinib ditosylate | BMS-690514 | Erlotinib-d6 hydrochloride | EGFR/CDK2-IN-1 | JBJ-04-125-02 | EGFR-IN-22 | EGFR-IN-34 | Epertinib | Ponezumab | Erlotinib Hydrochloride | EGFR-IN-36 | EGFR-IN-62 | Genistein | Panitumumab (anti-EGFR) | Lirafugratinib | Lapatinib-d7 dihydrochloride | (E/Z)-CP-724714 | TAS0728 | Rezivertinib | Tucatinib hemiethanolate | Osimertinib mesylate | AV-412 free base | Falnidamol | EGFR/ErbB-2/ErbB-4 inhibitor-2 | Trastuzumab | EGFR-IN-58 | Naquotinib | MS9449
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货号: HY-138751
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