Pyrazine is a heterocyclic aromatic organic compound with chemical formula C4H4N2. The marketed pyrazine drugs are mainly distributed in the field of anti-tumor and anti-infection. In recent years, there have been many new drugs in various fields, and there are some new target drugs worthy of attention.
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Existing BTK inhibitors directly bind to the active site of BTK and face challenges such as acquired resistance or incomplete responses over time. PROTAC-induced BTK degradation works as a novel alternative therapy for drug-resistant cancers. The latest journal Science publishes the identification of BTK mutations that are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127.
Nurix Therapeutics’ TPD compound NX-2127 is a first-in-class, dual-function small-molecule protein degrader. It drives targeted BTK and transcription factor IKAROS (IKZF1/3) degradation through ubiquitination and proteasomal degradation, adding combined benefit. NX-2127 is under development of phase I clinical trials that shows promising results and a manageable safety profile for the treatment of relapsed/ refractory B-cell malignancies.
Nurix announced the presentation of the first findings of clinical responses in the brain for NX-5948. NX-5948 is an investigational, orally bioavailable, brain penetrant, small molecule degrader of BTK. NX-5948 is currently being evaluated in a Phase 1 clinical trial in patients with relapsed or refractory B cell malignancies.