Theliatinib 是一种ATP 竞争性、口服活性和高度选择性的EGFR抑制剂，Ki为 0.05 nM，IC50为 3 nM。它具有抗肿瘤活性，对EGFR T790M/L858R突变体的IC50值为 22 nM。它对EGFR的选择性是其他激酶的 50 倍以上。

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.

In vitro studies suggest that Theliatinib is a potent EGFR kinase inhibitor with good kinase selectivity.

In vivo data demonstrated broad spectrum anti-tumor activity via oral dosing in multiple xerographs such as A-431, Bcap-37 and Fadu. Two PDECX models with EGFR gene amplification (PDECX1T0326 and PDECX1T0950) were sensitive to theliatinib treatment demonstrating tumor regression of 32% and 75%, respectively.

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.

1353644-70-8

C25H26N6O2

442.523

席栗替尼;西利替尼;Theliatinib

DMSO:47 mg/mL (106.21 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years