Ixazomib Citrate (MLN9708)

Catalog No.S4432 Synonyms: Ninlaro

For research use only.

Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively.

Ixazomib Citrate (MLN9708) Chemical Structure

CAS No. 1239908-20-3

Selleck's Ixazomib Citrate (MLN9708) has been cited by 7 Publications

Purity & Quality Control

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Biological Activity

Description Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively.
Targets
20S proteasome β5 site [1]
(Cell-free assay)
20S proteasome β5 site [1]
(Cell-free assay)
20S proteasome β1 site [1]
(Cell-free assay)
20S proteasome β2 site [1]
(Cell-free assay)
0.93 nM(Ki) 3.4 nM 31 nM 3500 nM

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(193.37 mM)
Water Insoluble
Ethanol ''''100 mg/mL

Chemical Information

Molecular Weight 517.12
Formula

C20H23BCl2N2O9

CAS No. 1239908-20-3
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03770260 Suspended Drug: Ixazomib Citrate|Drug: Pevonedistat Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma National Cancer Institute (NCI) April 23 2019 Phase 1
NCT03422874 Withdrawn Drug: MLN9708|Drug: Nelfinavir Neoplasms|Lymphoma Dartmouth-Hitchcock Medical Center August 2016 Phase 1
NCT02582359 Recruiting Drug: MLN9708|Drug: Cytarabine|Drug: Daunorubicin Acute Myeloid Leukemia Massachusetts General Hospital|Millennium Pharmaceuticals Inc. January 2016 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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