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limertinib

CAS No. : 1934259-00-3

MCE 站：limertinib

产品活性：limertinib (ASK120067) 是一种有效的口服活性 EGFR^T790M 抑制剂 (IC₅₀:0.3 nM)，对 EGFR^WT(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 EGFRL858R/T790Mand EGFRT790Mresistant mutants with IC₅₀ values of 0.3 nM ａnd 0.5 nM, respectively, as well as the EGFR^exon19delsensitizing mutant (IC₅₀= 0.5 nM). The ₅₀of limertinib against wild-type EGFR (EGFR^WT) 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 IC₅₀values 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 (EGFR^WT), with IC₅₀values 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 (EGFR^L858R/T790M)even at low dosage (0.1-1 nM). Additionally, limertinib inhibits p-EGFR ａnd p-Akt ａnd p-erk inEGFRWT 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.

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