Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGFR T790M/L858R mutant, respectively.

EGFR (L858R/T790M):22 nM (IC50), EGFR:3 nM (IC50), EGFR:0.05 nM (Ki)

体外研究表明，Theliatinib是一种具有良好激酶选择性的强效EGFR激酶抑制剂。

在体内数据表明，Theliatinib通过口服在多个异种移植瘤模型中展现了广谱的抗肿瘤活性。具有EGFR基因扩增的两个PDECX模型（PDECX1T0326和PDECX1T0950）对theliatinib治疗敏感，分别显示了32%和75%的肿瘤退缩。

Seven- to nine week old NOD-SCID immunodeficient or BALB/cASlac-nu/nu male or female mice. Fresh tumor specimens from newly diagnosed patients were collected during surgery and separated into three parts for the following: (1) To prepare formalin fixed paraffin embedded (FFPE) sections; (2) For snap freezing in liquid nitrogen for DNA extraction and sequencing and (3) For subcutaneous implantation into NOD-SCID mice (P0) and subsequent passages in additional NOD-SCID or nude mice once the tumor size reached 800~1500 mm^3. After several consecutive in vivo passages, the PDECX models (P3~P7) were used to evaluate the anti-tumor efficacy of theliatinib or gefitinib or AZD4547.