A novel small molecule inhibitor of IRE1. It inhibits IRE1 endonuclease activity but not its kinase activity after endoplasmic reticulum stress1-3. It displays significant antimyeloma activity in model human MM xenografts1. Induces apoptosis in pancreatic cancer cells and displays growth inhibition in a clonogenic growth assay in soft agar as well as in a xenograft in vivo model of pancreatic cancer4. Active in vivo.
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