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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-ASK120067
ASK120067

Chemical Structure : ASK120067

CAS No.: 1934259-00-3

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ASK120067 (Limertinib, ASK 120067)

货号: PC-38347Not For Human Use, Lab Use Only.

ASK120067 (Limertinib) is a novel third-generation inhibitor of EGFR T790M (L858R/T790M IC50=0.3 nM, T790M IC50=0.5 nM), with selectivity over EGFR WT (IC50=6 nM).

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10 mg ￥1380 In stock
25 mg ￥2380 In stock
50 mg ￥3880 In stock
100 mg ￥5880 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ASK120067 (Limertinib) is a novel third-generation inhibitor of EGFR T790M (L858R/T790M IC50=0.3 nM, T790M IC50=0.5 nM), with selectivity over EGFR WT (IC50=6 nM).
ASK120067 potently inhibited the EGFR L858R/T790M and EGFR T790M resistant mutants, with IC50 of 0.3 nM and 0.5 nM, respectively, as well as the EGFR exon19del sensitizing mutant (IC50= 0.5 nM).
ASK120067 also displayed a favorable selectivity profile against a panel of 258 kinases.
ASK120067 selectively inhibits the growth of EGFR-mutant cell lines and induces apoptosis, with IC50 values of 12 nM, 6 nM and 2 nM against NCI-H1975, PC-9, and HCC827 cells, respectively.
ASK120067 dose-dependently inhibited EGF-induced EGFR L858R/T790M phosphorylation and consequent activation of the downstream molecules AKT and ERK in NCI-H1975 cells, with similar or even more effective potency than osimertinib.
ASK120067 (5, 10 mg/kg once daily) demonstrated profound and selective antitumor efficacy in EGFR-mutant xenograft models in vivo.

物理化学性质&存储条件

分子量 546.072
分子式 C29H32ClN7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-[5-[[5-Chloro-4-(2-naphthalenylamino)-2-pyrimidinyl]amino]-2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxyphenyl]-2-propenamide

参考文献

1. Zhang T, et al. Mol Cancer. 2020 May 13;19(1):90.

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