Ixazomib Citrate (MLN9708) Analogue

Catalog No.S2181 Batch:S218101

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Technical Data

Formula

C20H23BCl2N2O9
Molecular Weight 517.12 CAS No. 1201902-80-8
Solubility (25°C)* In vitro DMSO 103 mg/mL (199.18 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.)

Preparing Stock Solutions

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)

References

  • https://pubmed.ncbi.nlm.nih.gov/20160034/
  • https://pubmed.ncbi.nlm.nih.gov/21724551/
  • https://pubmed.ncbi.nlm.nih.gov/30601533/
  • https://patents.google.com/patent/WO2016165677A1/en?oq=WO+2016165677

Customer Product Validation

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).

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

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

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

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.

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

Selleck's Ixazomib Citrate (MLN9708) Analogue has been cited by 8 publications

Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862] PubMed: 39319271
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.