Potent inhibitor of wild-type and fusion ALK (IC50 = 1.9 nM) and RET (IC50 = 4.8 nM), but not ROS1 tyrosine kinase activity. Significantly reduces proliferation and induces apoptosis in NSCLC, however these tumors can become resistant by activating Yes-associated protein 1 (YAP1). Causes cell...
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Potent inhibitor of wild-type and fusion ALK (IC50 = 1.9 nM) and RET (IC50 = 4.8 nM), but not ROS1 tyrosine kinase activity. Significantly reduces proliferation and induces apoptosis in NSCLC, however these tumors can become resistant by activating Yes-associated protein 1 (YAP1). Causes cell death in glioblastoma cells via inhibition of STAT3, and prolongs the survival of mice harboring intracerebral GBM xenografts. Has been used to enable allogeneic stem cell transplantation in a patient with ALK-positive anaplastic large-cell lymphoma. Clinically useful anticancer agent
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