Molecular Weight(MW): 517.12
MLN9708 immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.
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LAT2 is degraded by proteasomes after treatment with alkylphospholipids. (A): 3-h treatment of NB4 cells before exposure to the proteasome inhibitor MG132 (10 M) prevented the reduction of LAT2 induced by 25 M ODPC. (B)(C): a similar effect was observed after exposure (30 min) of NB4 cells to the proteasome inhibitor MLN9708 (5 M) followed by treatment with 25 M ODPC (B) or 25 M perifosine (C).
Mol Cell Proteomics, 2012, 11(12): 1898-912. MLN9708 purchased from Selleck.
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|Description||MLN9708 immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.|
|Features||The 1st oral proteasome inhibitor in early stage clinical trials for Multiple Myeloma.|
MLN9708 is a selective, orally bioavailable, second-generation proteasome inhibitor. MLN9708 has a shorter proteasome dissociation half-life and improved pharmacokinetics, pharmacodynamics, and antitumor activity compared with bortezomib, which we believe plays an important role in its improved tissue distribution. MLN9708 has a larger blood volume distribution at steady state, and analysis of 20S proteasome inhibition and markers of the unfolded protein response confirms that MLN9708 has greater pharmacodynamic effects in tissues than bortezomib. MLN9708 is a second-generation small-molecule proteasome inhibitor being developed for the treatment of a broad range of human malignancies.  Upon exposure to aqueous solutions or plasma, MLN9708 rapidly hydrolyzes to its biologically active form MLN2238.  MLN2238 is the biologically active form of MLN9708. 
|In vivo||MLN9708 shows superior antitumor activity in both solid tumor and hematologic preclinical xenograft models when administered via multiple dosing routes and regimens.  Recent preclinical pharmacology studies shows that MLN9708 has a shorter proteasome dissociation half-life than bortezomib, as well as improved pharmacokinetics, pharmacodynamics, and antitumor activity in xenograft models  MLN9708 has shown antitumor efficacy in a wide range of tumor xenografts. |
Kinase assay:Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents according to the manufacturer's instructions. Luminescence is measured using a LEADseeker instrument.
|In vitro||DMSO||100 mg/mL (193.37 mM)|
|In vivo||0.5% hydroxyethyl cellulose||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01660997||Withdrawn||Multiple Myeloma||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||July 30, 2012||Phase 2|
|NCT02697383||Recruiting||Multiple Myeloma|High Risk Smoldering Multiple Myeloma||Memorial Sloan Kettering Cancer Center|Millennium Pharmaceuticals, Inc.||February 2016||Phase 1|
|NCT02582359||Not yet recruiting||Acute Myeloid Leukemia||Massachusetts General Hospital|Millennium Pharmaceuticals, Inc.||November 2015||Phase 1|
|NCT02477215||Recruiting||Multiple Myeloma||Parameswaran Hari|Medical College of Wisconsin||October 2015||Phase 1|Phase 2|
|NCT02586038||Recruiting||Multiple Myeloma||Silvio Aime|University of Turin, Italy||October 2015||Phase 2|
|NCT02384746||Recruiting||Breast Cancer||Dartmouth-Hitchcock Medical Center||March 2015||Phase 1|
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