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ASK120067
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ASK120067
CAS No. : 1934259-00-3
MCE 站:ASK120067
产品活性: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。ASK120067 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 ASK120067 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 ASK120067 against wild-type EGFR (EGFRWT) is 6 nM.ASK120067 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.ASK120067 (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, ASK120067 inhibits p-EGFR and p-Akt and p-erk in?EGFR?WT A431 cell until the concentration reaches 10 to 100 nM.
In Vivo: ASK120067 (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 ASK120067 causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib.
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