In vitro and in vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing.

doi:10.1158/1535-7163.MCT-13-0966

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Community

Back to search

Article

In vitro and in vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing.

Molecular cancer therapeutics - 1 Jun 2014

Tjin Tham Sjin Robert, Lee Kwangho, Walter Annette O, Dubrovskiy Aleksandr, Sheets Michael, Martin Thia St, Labenski Matthew T, Zhu Zhendong, Tester Richland, Karp Russell, Medikonda Aravind, Chaturvedi Prasoon, Ren Yixuan, Haringsma Henry, Etter Jeff, Raponi Mitch, Simmons Andrew D, Harding Thomas C, Niu Deqiang, Nacht Mariana, Westlin William F, Petter Russell C, Allen Andrew, Singh Juswinder

Abstract excerpt

Patients with non-small cell lung carcinoma (NSCLC) with activating mutations in epidermal growth factor receptor (EGFR) initially respond well to the EGFR inhibitors erlotinib and gefitinib. However, all patients relapse because of the emergence of drug-resistant mutations, with T790M mutations accounting for approximately 60% of all resistance. Second-generation irreversible EGFR inhibitors are effective...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Carcinoma, Non-Small-Cell Lung

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Cell Proliferation

Share to Clinical Trials as Topic

Share to Drug Resistance, Neoplasm

Share to ErbB Receptors

Share to In Vitro Techniques

Share to Neoplasm Recurrence, Local

Share to Xenograft Model Antitumor Assays

Source

Open in PubMed

Identifiers

PMID: 24723450
DOI: 10.1158/1535-7163.MCT-13-0966

Genes

EGFR

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

In vitro and in vivo characterization of irreversible mutant-selective EGFR inhibitors that are wild-type sparing.PMID 24723450Read ↗

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Semantic proximity Read ↗

Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer.Semantic proximity Read ↗

Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine⁷⁹⁰ → methionine⁷⁹⁰ mutant.Semantic proximity Read ↗

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Semantic proximity Read ↗

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.Semantic proximity Read ↗

EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors.Semantic proximity Read ↗

Fighting cancer drug resistance: Opportunities and challenges for mutation-specific EGFR inhibitors.Semantic proximity Read ↗

Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.Semantic proximity Read ↗

Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLCSemantic proximity Read ↗

Whacking a mole-cule: clinical activity and mechanisms of resistance to third generation EGFR inhibitors in EGFR mutated lung cancers with EGFR-T790M.Semantic proximity Read ↗

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.Semantic proximity Read ↗

Novel Selective and Potent EGFR Inhibitor that Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.