| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 47 mg/mL (106.21 mM), Sonication is recommended.
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| Keywords | Xiliertinib | Theliatinib | phosphorylation | orally | Inhibitor | inhibit | HMPL-309 | HMPL309 | HMPL 309 | HER1 | esophageal | ERK | ErbB-1 | Epidermal growth factor receptor | EGFR | cancer | ATP-competitive | anti-tumor | AKT |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Brigatinib | Genistein | Gefitinib |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
