Ixazomib Citrate (MLN9708) Analogue

For research use only.

Catalog No.S2181

1 publication

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.

Selleck's Ixazomib Citrate (MLN9708) Analogue has been cited by 1 publication

3 Customer Reviews

  • LAT2 is degraded by proteasomes after treatment with alkylphospholipids. (A): 3-h treatment of NB4 cells before exposure to the proteasome inhibitor MG132 (10 M) prevented the reduction of LAT2 induced by 25 M ODPC. (B)(C): a similar effect was observed after exposure (30 min) of NB4 cells to the proteasome inhibitor MLN9708 (5 M) followed by treatment with 25 M ODPC (B) or 25 M perifosine (C).

    Mol Cell Proteomics, 2012, 11(12): 1898-912. Ixazomib Citrate (MLN9708) Analogue purchased from Selleck.

    Effect of proteasome inhibitors on [3H]-ryanodine binding. Panel A. Specific [3H]-ryanodine binding was measured in whole ventricle homogenates obtained in controls (C, white bars), after 30 min of ischemia (I, black bars) or after 30 min of ischemia followed by 60 minutes of reperfusion (IR, grey bars). MG132 was perfused at 0.5 μmol/L before ischemia (red bar, I) or from the very start of reperfusion (red bar, R). Values represent the mean ± S.E.M of different heartsas indicated in each bar *: p< 0.05 vs control or vs I + MG132. Panel B. Specific [3H]-ryanodine binding measured in hearts with the indicated concentration of ixazomib (ixa) perfused before ischemia. Values represent the mean ± S.E.M of values obtained in different hearts as indicated in each bar. *: p< 0.05 vs control

    PLoS One, 2016, 11(8):e0161068. Ixazomib Citrate (MLN9708) Analogue purchased from Selleck.

  • Structure and IC50 determination of ixazomib. Results represent means of three independent biological replicates, error bars indicate standard deviations. Smears were stained using DiffQuik staining set, parasitemia was counted at 1000 RBCs. Statistical analysis was performed in R using ANOVA. * = p < 0.05, *** = p < 0.001 (compared to the DMSO treated culture). Experimental conditions: starting parasitemia 2% (dotted line), medium with inhibitory compounds exchanged in 12 h intervals, total cultivation duration 48 h. DC: DMSO treated culture (0.008%). UC: untreated culture. IC50: half maximal inhibitory concentration. RBCs: red blood cells.

    Int J Parasitol Drugs Drug Resist, 2018, 8(3):394-402. Ixazomib Citrate (MLN9708) Analogue purchased from Selleck.

Purity & Quality Control

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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)
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% DMSO % % Tween 80 % ddH2O
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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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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 SDS / 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 SDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

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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

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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
NCT01936532 Active not recruiting Drug: MLN9708|Drug: Lenalidomide|Drug: Dexamethasone Newly Diagnosed Multiple Myeloma Nantes University Hospital November 12 2014 Phase 2
NCT02168101 Completed Drug: MLN9708 Multiple Myeloma SCRI Development Innovations LLC|Millennium Pharmaceuticals Inc. September 2014 Phase 2

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID