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AdipoGen Ixazomib citrate MLN9708
Supplier: AdipoGen AGCR13671M001
Chemical. CAS 1239908-20-3. Formula C20H23BCl2N2O9. MW 517.1. Synthetic. Potent selective and reversible proteasome inhibitor all proteolytic subunits. Targets the chymotrypsin-like beta5 subunit of the constitutive 20S proteasome IC50=3.4nM. Cross-reacts and inhibits the trypsin-like beta2 subunit IC50=3.5µM and the caspase-like/peptidyl-glutamyl peptide-hydrolyzing PGPH beta1 subunit IC50=0.03µM. Anticancer compound effective in cell-based assays, in xenografts and against multiple myeloma in vivo. In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma. Prodrug that rapidly hydrolyzes to MLN2238 AG-CR1-3670. Exhibits improved pharmacodynamics and antitumor activity compared to bortezomib in various B-cell lymphoma models, due to a greater tumor to blood ratio of proteasome inhibition that ultimately translates into improved tumor pharmacodynamic response and antitumor activity in several tumor xenograft models.
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