Formulation: A crystalline solid
Formal Name: B-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]-boronic acid
Purity: ≥95%
Formula Markup: C14H19BCl2N2O4
Formula Weight: 361
Shelf life (days): 1460
CAS Number: 1072833-77-2
Notes: MLN2238 is an inhibitor of the β5 subunit of the 20S proteasome (IC50 = 3.4 nM in a cell-free assay) and an active metabolite of MLN9708 (Item No. 18386).{31628,31627} It is formed from MLN9708 via hydrolysis in plasma.{31628} MLN2238 is selective for the chymotrypsin-like β5 subunit over the caspase-like β1 and trypsin-like β2 subunits (IC50s = 31 and 3,500 nM, respectively). It also binds caseinolytic protease P (Kd = 5,700 nM) and prevents hemolysis of isolated ovine erythrocytes induced by methicillin-resistant S. aureus (MRSA; EC50 = 3,600 nM).{58924} MLN2238 inhibits the proliferation of A375 and H460 lung and HCT116 and HT-29 colon cancer cells (IC50s = 20, 58, 19, and 52 nM, respectively) as well as osteoclastogenesis in peripheral blood mononuclear cells (PBMCs) isolated from patients with multiple myeloma (IC50 = 4.8 nM).{31628,31627} It reduces tumor growth in a CWR22 prostate cancer mouse xenograft model when administered at a dose of 14 mg/kg. Formulations containing MLN2238 have been used in the treatment of multiple myeloma.
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