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。

limertinib (ASK120067) is a potent and orally active inhibitor of EGFR (IC 50 :0.3 nM) with selectivity over EGFR (IC 50 :6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC).

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EGFR 0.5 nM (IC50) EGFR 0.3 nM (IC50

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 EGFR sensitizing mutant (IC50= 0.5 nM). The 50 of limertinib against wild-type EGFR (EGFR) 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 (EGFR), with IC50 values ranging from 338 nM to 1541 nM.
limertinib (0.1-100 nM) inhibits the phosphorylation o

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Tao Zhang, et al. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90.

In Vitro: DMSO : 41.67 mg/mL (76.31 mM; Need ultrasonic)配制储备液