Discover Community Create You

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

Article

Pan-KRAS Inhibitors BI-2493 and BI-2865 Display Potent Antitumor Activity in Tumors with KRAS Wild-type Allele Amplification.

Molecular cancer therapeutics - 2 Apr 2025

Tedeschi Antonio, Schischlik Fiorella, Rocchetti Francesca, Popow Johannes, Ebner Florian, Gerlach Daniel, Geyer Antonia, Santoro Valeria, Boghossian Andrew S, Rees Matthew G, Ronan Melissa M, Roth Jennifer A, Lipp Jesse, Samwer Matthias, Gmachl Michael, Kraut Norbert, Pearson Mark, Rudolph Dorothea

Abstract excerpt

KRASG12C selective inhibitors, such as sotorasib and adagrasib, have raised hopes of targeting other KRAS-mutant alleles in patients with cancer. We report that KRAS wild-type (WT)-amplified tumor models are sensitive to treatment with the small-molecule KRAS inhibitors BI-2493 and BI-2865. These pan-KRAS inhibitors directly target the "OFF" state of KRAS and result in potent antitumor activity in preclinical...

Read the complete abstract on PubMed

Topics

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

Share to Blood disorders and treatments
Share to Chronic Lymphocytic Leukemia Research

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Share to Protein Kinase Regulation and GTPase Signaling

Source

Open in PubMed Open full text

Identifiers

PMID: 39711431
DOI: 10.1158/1535-7163.MCT-24-0386
PMCID: PMC11962398

Genes

KRAS

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 30 Oct 2026.

Related research

Semantic proximity does not establish scientific evidence. Graph snapshot: 2026-09-29.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Pan-KRAS Inhibitors BI-2493 and BI-2865 Display Potent Antitumor Activity in Tumors with KRAS Wild-type Allele AmplificationPMID 39711431Read ↗

Combinations of RAS pathway inhibitors with targeted agents are active in spheroids of patient-derived cells with oncogenic KRAS variants from multiple cancer typesSemantic proximity Read ↗

Expanding the Reach of Precision Oncology by Drugging All KRAS Mutants.Semantic proximity Read ↗

Unlocking KRAS: Navigating Its Molecular Biology and Treatment Landscape Among Gastrointestinal Malignancies.Semantic proximity Read ↗

Genomic landscape of clinically acquired resistance alterations in patients treated with KRASG12C inhibitors.Semantic proximity Read ↗

State-of-the-art and upcoming trends in RAS-directed therapies in gastrointestinal malignancies.Semantic proximity Read ↗

Precision Targeting of KRAS-Mutant Cancers: Beyond G12C Toward G12D and Pan-RAS Therapeutic Strategies.Semantic proximity Read ↗

Recent advances in therapeutic targeting of the KRAS pathway in cancer.Semantic proximity Read ↗

Expanding Addressable KRAS Mutations through the Structure- and Property-Based Design of Dual-State (GDP/GTP), Reversible Pan-KRAS Inhibitors.Semantic proximity Read ↗

BI-3406, a Potent and Selective SOS1-KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition.Semantic proximity Read ↗

[Therapeutic Strategies Targeting the KRAS G12C Mutation-Current Landscape and Future Directions].Semantic proximity Read ↗

The Next Generation of KRAS Targeting: Reasons for Excitement and Concern.Semantic proximity Read ↗

Landscape of KRAS G12C , Associated Genomic Alterations, and Interrelation With Immuno-Oncology Biomarkers in KRAS -Mutated CancersSemantic proximity Read ↗

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