| Name | Theliatinib |
| Description | 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. |
| Animal Research | 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. |
| In vitro | In vitro studies suggest that Theliatinib is a potent EGFR kinase inhibitor with good kinase selectivity. |
| In vivo | 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 47 mg/mL (106.21 mM)
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| Keywords | ATP-competitive | inhibit | EGFR | ERK | cancer | esophageal | Epidermal growth factor receptor | HMPL-309 | anti-tumor | Inhibitor | ErbB-1 | HMPL309 | HER1 | HMPL 309 | Theliatinib | orally | Xiliertinib | AKT | phosphorylation |
| Inhibitors Related | Osimertinib | Lapatinib | Erlotinib | Gefitinib |
| Related Compound Libraries | 经典已知活性库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 已知活性化合物库 | 抗癌活性化合物库 |
United States
