Ixazomib citrate
Based on 6 publication(s) in Google Scholar
Ixazomib citrate (MLN9708) is a selective, orally active, second-generation proteasome inhibitor. Ixazomib citrate can be used for the study of a broad range of human malignancies.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 1239908-20-3
- Formula: C20H23BCl2N2O9
- Molecular Weight:517.12
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ixazomib citrate
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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WB
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WB
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WB
Biological Activity
IC50: 3.4 nM (20S proteasome β5), 31 nM (20S proteasome β1), 3500 nM (20S proteasome β2)[3]
Ixazomib citrate (MLN9708; 0.20-3.20 μM) inhibits the cell growth of both cell lines effectively in a time- and dose-dependent manner. Ixazomib induces cell cycle arrest in MG-63 and Saos-2 cells. Ixazomib induces apoptosis mainly through the caspases pathway and requires the activation of both caspase8 and caspase9. Ixazomib treatment increases the levels of pro-apoptotic proteins and down regulates the anti-apoptotic proteins that control MOMP. Ixazomib treatment induces the release of Cytc, Smac, OMI from mitochondria and decreases the protein levels of XIAP. Ixazomib inhibits the invasion ability of MG-63 and Saos-2 cells and decreases both the expression and secretion levels of MMP2/9[1].Ixazomib citrate (MLN9708; 12 nM) shows inhibitory activity against C-L and T-L proteasome activities. Treatment of H929 and MM.1S MM cells with Ixazomib triggers a marked increase in proteolytic cleavage of poly(ADP) ribose polymerase (PARP), a signature event during apoptosis. Ixazomib induces cleavage of caspase-3, an upstream activator of PARP. Ixazomib induces eIf2-α kinase activity and protein levels of Bip and CHOP/GADD153. Ixazomib blocks BMSCs-induced MM cell proliferation, inhibits in vitro capillary tubule formation, and target NF-κB[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1239908-20-3
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Appearance Solid
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Molecular Weight 517.12
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Formula C20H23BCl2N2O9
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Color White to off-white
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SMILES
O=C(O)CC1(CC(O)=O)OB([C@@H](NC(CNC(C2=CC(Cl)=CC=C2Cl)=O)=O)CC(C)C)OC1=O
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Synonyms
MLN9708
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Chem Biol
2022 Mar 17;29(3):386-397.e9. PMID: 34469831
Ixazomib citrate purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2022 Mar 17;29(3):386-397.e9. [Abstract]
Immunoblots for NSD3S using the indicated cells pre-treated with DMSO, 10 nM of Lxazomib citrate (MLN9708) for two hours, followed by a 48-hour treatment with 5 μM of MS9715.
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J Med Chem
Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos. [Abstract]2022 Aug 11;65(15):10611-10625. PMID: 35895319
Ixazomib citrate purchased from MedChemExpress. Usage Cited in: J Med Chem. 2022 Aug 11;65(15):10611-10625. [Abstract]
Compound 9 (MS159, NSD2 PROTAC degrader) reduces the IKZF3 protein level in 293FT cells in a proteasome-dependent manner. 293FT cells were pretreated with DMSO, 10 nM of Lxazomib citrate (MLN9708) or 0.5 μM of MLN4924 for 2 h, followed by a 6 h treatment with 5 μM of compound 9.
Ixazomib citrate purchased from MedChemExpress. Usage Cited in: J Med Chem. 2022 Aug 11;65(15):10611-10625. [Abstract]
Compound 9 (MS159, NSD2 PROTAC degrader) reduces the IKZF1 and IKZF3 protein levels in KMS11 cells in a proteasome-dependent manner. KMS11 cells were pretreated with DMSO, 10 nM of Lxazomib citrate (MLN9708) or 0.5 μM of MLN4924 for 2 h, followed by a 6 h treatment with 5 μM of compound 9. The IKZF1 and IKZF3 protein levels were detected by Western blotting with GAPDH as the loading control.
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Ixazomib citrate purchased from MedChemExpress. Usage Cited in: Patent. US20240212786A1.
Showed dose-response curves of ixazomib citrate in four LIHC cell lines (SNU-398, Huh7, SK-Hep-1 and HepG2).
Ixazomib citrate purchased from MedChemExpress. Usage Cited in: Patent. US20240212786A1.
Showed schematic view of prolonged colony assay (Left). Negative effect of Ixazomib citrate on the colony formation assay in four LIHC cell lines: SNU-398, Huh7, SK-Hep-1, and HepG2 (Right).
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Solvent & Solubility
DMSO : 250 mg/mL (483.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.02 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cell viability is assessed using the MTT assay. Cells are trypsinized and seeded in 96-well plate at 5000 cells per well. Cells are treated with Ixazomib or DMSO in basal medium at the indicated doses and times. Cell viability is determined relative to control cells treated with vehicle alone.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ixazomib is dissolved in 5% 2-hydroxypropyl-β- cyclodextrin at 2 mg/mL concentration. The human plasmacytoma xenograft tumor model is used in the assay. CB-17 SCID mice (n=21) are subcutaneously inoculated with 5.0×106 MM.1S cells in 100 µL serum-free RPMI-1640 medium, and randomized to treatment groups when tumors reach 250-300 mm3. Mice are treated with vehicle, bortezomib (1 mg/kg; i.v) or Ixazomib (11 mg/kg; i.v) twice weekly for 3 weeks. Animals are euthanized when their tumors reach 2 cm3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9338 mL | 9.6689 mL | 19.3379 mL | 48.3447 mL |
| 5 mM | 0.3868 mL | 1.9338 mL | 3.8676 mL | 9.6689 mL | |
| 10 mM | 0.1934 mL | 0.9669 mL | 1.9338 mL | 4.8345 mL | |
| 15 mM | 0.1289 mL | 0.6446 mL | 1.2892 mL | 3.2230 mL | |
| 20 mM | 0.0967 mL | 0.4834 mL | 0.9669 mL | 2.4172 mL | |
| 25 mM | 0.0774 mL | 0.3868 mL | 0.7735 mL | 1.9338 mL | |
| 30 mM | 0.0645 mL | 0.3223 mL | 0.6446 mL | 1.6115 mL | |
| 40 mM | 0.0483 mL | 0.2417 mL | 0.4834 mL | 1.2086 mL | |
| 50 mM | 0.0387 mL | 0.1934 mL | 0.3868 mL | 0.9669 mL | |
| 60 mM | 0.0322 mL | 0.1611 mL | 0.3223 mL | 0.8057 mL | |
| 80 mM | 0.0242 mL | 0.1209 mL | 0.2417 mL | 0.6043 mL | |
| 100 mM | 0.0193 mL | 0.0967 mL | 0.1934 mL | 0.4834 mL |
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