2. Metabolic Enzyme/Protease Autophagy
  3. Proteasome Autophagy
  4. Ixazomib citrate

Ixazomib citrate  (Synonyms: MLN9708)

Cat. No.: HY-10452 Purity: 99.89%
COA Handling Instructions

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Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.

For research use only. We do not sell to patients.

Ixazomib citrate Chemical Structure

Ixazomib citrate Chemical Structure

CAS No. : 1239908-20-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 63 In-stock
Solution
10 mM * 1 mL in DMSO USD 63 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 77 In-stock
50 mg USD 165 In-stock
100 mg USD 275 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Ixazomib citrate:

Ixazomib citrate Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.

IC50 & Target

IC50: 3.4 nM (20S proteasome β5), 31 nM (20S proteasome β1), 3500 nM (20S proteasome β2)[3]
In Vitro

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.

Ixazomib citrate Related Antibodies
In Vivo

Ixazomib citrate (MLN9708; 11 mg/kg) significantly inhibits MM tumor growth and prolongs survival in the human plasmacytoma MM.1S xenograft mouse model. The blood chemistry profiles of Ixazomib-treated mice show normal levels of creatinine, hemoglobin, and bilirubin. Ixazomib dramatically increases the number of cleaved-caspase-3 positive cells of the xenograft model[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

517.12

Formula

C20H23BCl2N2O9
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9338 mL 9.6689 mL 19.3379 mL
5 mM 0.3868 mL 1.9338 mL 3.8676 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.89%

COA (251 KB) HNMR (153 KB) LCMS (258 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
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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Ixazomib citrate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ixazomib1239908-20-3MLN9708MLN 9708MLN-9708ProteasomeAutophagyInhibitorinhibitorinhibit

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