An orally bioavailable prodrug of the second-generation proteasome inhibitor MLN2239

MLN9708 – 50 mg

Brand:
Cayman
CAS:
1201902-80-8
Storage:
-20
UN-No:
Non-Hazardous - /

MLN9708 is an orally bioavailable prodrug of the second-generation proteasome inhibitor MLN2239 (Item No. 18385).{31628,31627} This prodrug rapidly hydrolyzes in plasma to the biologically active form, which inhibits the β5 chymotryptic-like subunit of the 20S proteasome (IC50 = 3.4 nM; Ki = 0.93 nM in cell-free assays).{31628,31627} It inhibits the β1 caspase-like and β2 trypsin-like proteolytic sites with IC50 values of 0.03 and 3.5 µM, respectively.{31628} MLN9708 has shown antitumor activity both in cell-based assays and in xenograft models and has been examined in phase III clinical trials for potential antimyeloma activity.{31628,31627}  

 

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Description

An orally bioavailable prodrug of the second-generation proteasome inhibitor MLN2239, which inhibits the β5 chymotryptic-like subunit of the 20S proteasome (IC50 = 3.4 nM; Ki = 0.93 nM)

Formal name: 4-carboxy-2-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]-6-oxo-1,3,2-dioxaborinane-4-acetic acid

Synonyms:  Ixazomib Citrate

Molecular weight: 517.1

CAS: 1201902-80-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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