Home Proteases Proteasome inhibitor - Autophagy activator Ixazomib Citrate (MLN9708) Analogue For research use only.

Ixazomib Citrate (MLN9708) Analogue

Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (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. Ixazomib (MLN2238) induces autophagy. Phase 3.

Ixazomib Citrate (MLN9708) Analogue Chemical Structure

Ixazomib Citrate (MLN9708) Analogue Chemical Structure

CAS: 1201902-80-8

Selleck's Ixazomib Citrate (MLN9708) Analogue has been cited by 6 Publications

3 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.70%
99.70

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Biological Activity

Description Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (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. Ixazomib (MLN2238) induces autophagy. Phase 3.
Targets
20S proteasome [1]
(Cell-free assay)		 20S proteasome [1]
(Cell-free assay)
0.93 nM(Ki) 3.4 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03422874 Withdrawn Neoplasms|Lymphoma Dartmouth-Hitchcock Medical Center August 2016 Phase 1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
NCT01936532 Completed Newly Diagnosed Multiple Myeloma Nantes University Hospital November 12 2014 Phase 2
NCT02168101 Completed Multiple Myeloma SCRI Development Innovations LLC|Millennium Pharmaceuticals Inc. September 2014 Phase 2

Chemical lnformation & Solubility

Molecular Weight 517.12 Formula

C20H23BCl2N2O9
CAS No. 1201902-80-8 SDF Download Ixazomib Citrate (MLN9708) Analogue SDF
Smiles B1(OC(=O)CC(O1)(CC(=O)O)C(=O)O)C(CC(C)C)NC(=O)CNC(=O)C2=C(C=CC(=C2)Cl)Cl
Storage (From the date of receipt)

In vitro
Batch:

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

Water : Insoluble

Ethanol : 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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