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

Meredith S. Eno, Jason D. Brubaker, John E. Campbell, +25

Journal of Medicinal Chemistry

Adenosine Signaling Is Prognostic for Cancer Outcome and Has Predictive Utility for Immunotherapeutic Response

Ben Sidders, Pei Zhang, Kelly Goodwin, +16

Clinical Cancer Research

Potent and selective pyrazole-based inhibitors of B-Raf kinase

Joshua D. Hansen, Jonas Grina, Brad Newhouse, +14

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryB-raf KinaseMedicineRational Drug DesignPharmacotherapy +4

1296P BLU-945, a highly potent and selective 4th generation EGFR TKI for the treatment of EGFR T790M/C797S resistant NSCLC

Stefanie S. Schalm, Tom Dineen, Sangbin Lim, +16

Annals of Oncology

Drug TargetingMedicineSelective 4ThGeneration Egfr TkiPharmacotherapy +4

Non-oxime pyrazole based inhibitors of B-Raf kinase

Bradley J. Newhouse, Joshua D. Hansen, Jonas Grina, +14

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicineMechanism Of ActionAnti-cancer AgentPharmacology +2

Potent and Selective Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors. 1. 4-(4-Bromo-2-fluorophenylamino)-1- methylpyridin-2(1<i>H</i>)-ones

Eli M. Wallace, Joseph P. Lyssikatos, James F. Blake, +14

Journal of Medicinal Chemistry

Mek 1,2Selective InhibitorsPharmacotherapyCancer BiologyPharmaceutical Chemistry +19

The effect of lithium on the membrane molecular dynamics of normal human erythrocytes

Jay W. Pettegrew, Jacob Short, Rich Woessner, +5

Biological Psychiatry

Molecular PhysiologyNormal Human ErythrocytesCell DivisionOrganelle DynamicMembrane Transport +9

Abstract 1262: BLU-701 is a highly potent, brain-penetrant and WT-sparing next-generation EGFR TKI for the treatment of sensitizing (ex19del, L858R) and C797S resistance mutations in metastatic NSCLC

Chiara Conti, John Campbell, Rich Woessner, +23

Cancer Research

Metastatic NsclcPathologyKinase InhibitorsC797s Resistance MutationsTumor Biology +19

Abstract #1795: In Vitro and in vivo activity of ARRY-380: A potent, small molecule inhibitor of ErbB2.

Tracy Pheneger, Karyn Bouhana, Deborah Anderson, +17

Cancer Research

Small Molecule InhibitorPharmacotherapyTumor BiologyTranslational PharmacologyMolecular Pharmacology +18

Abstract 1467: BLU-945, a fourth-generation, potent and highly selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with intracranial activity, demonstrates robust <i>in vivo</i> antitumor activity in models of osimertinib-resistant non-small cell lung cancer (NSCLC)

Sun Min Lim, Chae Won Park, Zhuo Zhang, +14

Cancer Research

Lung AdenocarcinomaPathologyAbstract 1467Resistance MutationsCancer Biology +18