Discovery of CH7057288 as an Orally Bioavailable, Selective, and Potent pan-TRK Inhibitor.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01099
Abstract: Kinase fusions involving tropomyosin receptor kinases (TRKs) have been proven to act as strong oncogenic drivers and are therefore recognized as attractive therapeutic targets. We screened an in-house kinase-focused library and identified a promising hit… read more here.
Keywords: selective potent; orally bioavailable; bioavailable selective; trk inhibitor ... See more keywords
Demonstration of an anti‐hyperalgesic effect of a novel pan‐Trk inhibitor PF‐06273340 in a battery of human evoked pain models
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DOI: 10.1111/bcp.13448
Abstract: AIM Inhibitors of nerve growth factor (NGF) reduce pain in several chronic pain indications. NGF signals through tyrosine kinase receptors of the tropomyosin-related kinase (Trk) family and the unrelated p75 receptor. PF-06273340 is a small… read more here.
Keywords: pan trk; trk inhibitor; inhibitor; primary endpoints ... See more keywords
Abstract 3727: Plasma inhibitory activity (PIA) is a possible pharmacodynamic marker for clinical development of a next generation pan-TRK inhibitor, ONO-5390556
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DOI: 10.1158/1538-7445.am2017-3727
Abstract: Background: Colorectal cancer and Mammary analogue secretory carcinoma harboring Neurotrophic tyrosine receptor kinase (NTRK/TRK) gene rearrangements developed resistance to Entrectinib, ALK/ROS/TRK inhibitor. We previously demonstrated that the next generation pan-TRK inhibitor,ONO-5390556 may potently overcome Entrectinib-resistance… read more here.
Keywords: ono 5390556; inhibition trk; trk inhibitor; pia ... See more keywords
Abstract 4179: Potent and selective TRK inhibitor CH7057288
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-4179
Abstract: TRK receptor tyrosine kinases are expressed as fusion proteins encoded by various fusion genes across a wide variety of cancer types, including lung and colorectal cancer. These fusion proteins have potent oncogenic activity and are… read more here.
Keywords: trk inhibitor; potent selective; inhibitor; trk ... See more keywords
JND4135, a New Type II TRK Inhibitor, Overcomes TRK xDFG and Other Mutation Resistance In Vitro and In Vivo
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DOI: 10.3390/molecules27196500
Abstract: The tropomyosin receptor kinases (TRKs) have been validated as effective targets in anticancer drug discovery. Two first-generation TRK inhibitors have been approved into market and displayed an encouraging therapeutic response in cancer patients harboring TRK… read more here.
Keywords: jnd4135 new; trk; resistance; trk inhibitor ... See more keywords