The BTK inhibitor ARQ 531 targets ibrutinib-resistant CLL and Richter transformation
SD Reiff, R Mantel, LL Smith, JT Greene, EM Muhowski… - Cancer discovery, 2018 - AACR
Targeted inhibition of Bruton tyrosine kinase (BTK) with the irreversible inhibitor ibrutinib has
improved outcomes for patients with hematologic malignancies, including chronic
lymphocytic leukemia (CLL). Here, we describe preclinical investigations of ARQ 531, a
potent, reversible inhibitor of BTK with additional activity against Src family kinases and
kinases related to ERK signaling. We hypothesized that targeting additional kinases would
improve global inhibition of signaling pathways, producing more robust responses. In vitro …
improved outcomes for patients with hematologic malignancies, including chronic
lymphocytic leukemia (CLL). Here, we describe preclinical investigations of ARQ 531, a
potent, reversible inhibitor of BTK with additional activity against Src family kinases and
kinases related to ERK signaling. We hypothesized that targeting additional kinases would
improve global inhibition of signaling pathways, producing more robust responses. In vitro …
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