产品
编 号：F762424
分子式：C29H32ClN7O2
分子量：546.06
分子式：C29H32ClN7O2
分子量：546.06
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规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1934259-00-3
产品详情
生物活性：
limertinib (ASK120067) is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of?non-small cell lung cancer (NSCLC).
体内研究：
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.Animal Model:BALB/cA nude mice
Dosage:5-20 mg/kg
Administration:Oral gavage; 5-20 mg/kg; once daily; 21 days
Result:Were well tolerated in animals without observed body weight lossDemonstrated profound and selective antitumor efficacy and decreased TGI rate.Significantly inhibited the phosphorylation of EGFR?L858R/T790M?and AKT in tumor tissue.
体外研究：
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.
limertinib (ASK120067) is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of?non-small cell lung cancer (NSCLC).
体内研究：
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.Animal Model:BALB/cA nude mice
Dosage:5-20 mg/kg
Administration:Oral gavage; 5-20 mg/kg; once daily; 21 days
Result:Were well tolerated in animals without observed body weight lossDemonstrated profound and selective antitumor efficacy and decreased TGI rate.Significantly inhibited the phosphorylation of EGFR?L858R/T790M?and AKT in tumor tissue.
体外研究：
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.
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