Ixazomib Citrate (MLN9708) Analogue

For research use only.

Catalog No.S2181

Ixazomib Citrate (MLN9708) Analogue Chemical Structure

CAS No. 1201902-80-8

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.

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10mM (1mL in DMSO) USD 350 In stock
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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

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (193.37 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% hydroxyethyl cellulose
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 517.12
Formula

C20H23BCl2N2O9

CAS No. 1201902-80-8
Storage powder
in solvent
Synonyms N/A
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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
NCT02250300 Completed Drug: MLN9708 Allogeneic Hematopoietic Stem Cell Transplantation Mehdi Hamadani|Medical College of Wisconsin November 19 2014 Phase 1|Phase 2
NCT02168101 Completed Drug: MLN9708 Multiple Myeloma SCRI Development Innovations LLC|Millennium Pharmaceuticals Inc. September 2014 Phase 2
NCT02042989 Active not recruiting Drug: MLN9708|Drug: Vorinostat Advanced Cancers M.D. Anderson Cancer Center|Millennium Pharmaceuticals Inc. June 27 2014 Phase 1

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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID