limertinib (ASK120067) is a potent and orally active inhibitor ofEGFR^T790M(IC₅₀:0.3 nM) with selectivity overEGFR^WT(IC₅₀:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lungcancer(NSCLC)^[1].

In thein vitrokinase assay limertinib potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC₅₀values of 0.3 nM and 0.5 nM, respectively, as well as the EGFR^exon19del sensitizing mutant (IC₅₀= 0.5 nM). The₅₀ of limertinib against wild-type EGFR (EGFR^WT) is 6 nM^[1].
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^WT), with IC₅₀ values ranging from 338 nM to 1541 nM^[1].
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 in EGFR WTA431 cell until the concentration reaches 10 to 100 nM^[1].

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^[1].

546.06

Solid

C₂₉H₃₂ClN₇O₂

1934259-00-3

Room temperature in continental US; may vary elsewhere.

DMSO : 41.67 mg/mL(76.31 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (4.58 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.81 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。