Ixazomib Citrate (MLN9708) Analogue

Catalog No.S2181 Batch:S218103

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Technical Data

Formula

C20H23BCl2N2O9
Molecular Weight 517.12 CAS No. 1201902-80-8
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)
Homogeneous suspension
0.5% hydroxyethyl cellulose
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% hydroxyethyl cellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Customer Product Validation

Data from [Data independently produced by , , Mol Cell Proteomics, 2012, 11(12): 1898-912]

Data from [Data independently produced by , , PLoS One, 2016, 11(8):e0161068]

Data from [Data independently produced by , , Int J Parasitol Drugs Drug Resist, 2018, 8(3):394-402]

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

Loss of TDP-43 oligomerization or RNA binding elicits distinct aggregation patterns [ EMBO J, 2023, 42(17):e111719] PubMed: 37431963
A Drosophila model of diabetic neuropathy reveals a role of proteasome activity in the glia [ iScience, 2023, 26(6):106997] PubMed: 37378316
TRPA1 promotes melanosome phagocytosis in keratinocytes via PAR-2/CYLD axis [ J Dermatol Sci, 2022, S0923-1811(22)00125-6] PubMed: 35637111
HAPLN1 confers multiple myeloma cell resistance to several classes of therapeutic drugs [ PLoS One, 2022, 17(12:e0274704)] PubMed: 36480501
LAMP3 inhibits autophagy and contributes to cell death by lysosomal membrane permeabilization [ Autophagy, 2021, 1-19] PubMed: 34802379
Synergistic PIM kinase and proteasome inhibition as a therapeutic strategy for MYC-overexpressing triple-negative breast cancer [ Cell Chem Biol, 2021, S2451-9456(21)00400-1] PubMed: 34525344
High Immunoproteasome Activity and sXBP1 in Pediatric Precursor B-ALL Predicts Sensitivity towards Proteasome Inhibitors [ Cells, 2021, 10(11)2853] PubMed: 34831075

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.