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EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor.
Non-small cell lung cancer patients carrying oncogenic EGFR mutations initially respond to EGFR-targeted therapy, but later elicit minimal response due to dose-limiting toxicities and acquired… Expand
EC144 is a potent inhibitor of the heat shock protein 90.
- J. Shi, R. Van de Water, +26 authors M. Biamonte
- Chemistry, Medicine
- Journal of medicinal chemistry
- 31 August 2012
Alkyne 40, 5-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-2-methylpent-4-yn-2-ol (EC144), is a second generation inhibitor of heat shock protein… Expand
Combined ALK and MDM2 inhibition increases antitumor activity and overcomes resistance in human ALK mutant neuroblastoma cell lines and xenograft models
The efficacy of ALK inhibitors in patients with ALK-mutant neuroblastoma is limited, highlighting the need to improve their effectiveness in these patients. To this end, we sought to develop a… Expand
BIIB021 is a small molecule inhibitor of the heat shock protein, Hsp90, that shows potent anti-tumor activity in preclinical models
B161 Hsp90 is a widely-expressed molecular chaperone that functions in the maturation and stabilization of cellular proteins. Complexed together with other co-chaperone proteins, Hsp90 catalyzes the… Expand
EGF816, an irreversible mutant-selective EGFR inhibitor, is effective in NSCLC with both primary activating and T790M-mediated resistant EGFR mutations
NSCLC patients carrying oncogenic EGFR mutations initially respond to EGFR targeted therapy. However, duration of the response is limited due to dose limiting toxicities and acquired resistance.… Expand
Abstract B35: Validation of a multiplex method for detection of several oncosignaling proteins with potential utility for assessment of pharmacodynamic activity of hsp90 inhibitors
Biomarkers are increasingly being used in early phase clinical trials not only to determine pharmacodynamic activity but also as surrogate end points of clinical efficacy. BIIB021 is a synthetic… Expand