Ixazomib Citrate (MLN9708)

Ixazomib Citrate (MLN9708) 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

Ixazomib Citrate (MLN9708) Chemical Structure

CAS: 1239908-20-3

Selleck's Ixazomib Citrate (MLN9708) has been cited by 10 publications

Purity & Quality Control

Batch: Purity: 99.96%
99.96

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Biological Activity

Description Ixazomib Citrate (MLN9708) 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05882279 Completed Multiple Myeloma Takeda June 1 2023 --
NCT03422874 Withdrawn Neoplasms|Lymphoma Dartmouth-Hitchcock Medical Center August 2016 Phase 1
NCT02582359 Completed Acute Myeloid Leukemia Massachusetts General Hospital|Millennium Pharmaceuticals Inc. January 2016 Phase 1

Chemical lnformation & Solubility

Molecular Weight 517.12 Formula

C20H23BCl2N2O9

CAS No. 1239908-20-3 SDF --
Smiles CC(C)CC(NC(=O)CNC(=O)C1=C(Cl)C=CC(=C1)Cl)B2OC(=O)C(CC(O)=O)(CC(O)=O)O2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (193.37 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

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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.

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