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Ixazomib Citrate (MLN9708) Proteasome inhibitor

Name: Ixazomib Citrate (MLN9708)
Brand: Selleck Chemicals
SKU: S4432
Availability: InStock
Rating: 5 (12 reviews)

Cat.No.S4432

Ixazomib Citrate (MLN9708) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively.

Chemical Structure

Molecular Weight: 517.12

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	HDAC Caspase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease Serine Protease Secretase PCSK9 Glutaminase Acyltransferase Thrombin Cathepsin B MALT PAD PREP Neprilysin SGK Aminopeptidase 3C-Like Protease PGDS GOT
Related Products	MG132 Epoxomicin (BU-4061T) Celastrol Oprozomib ONX-0914 (PR-957) Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840 Isoginkgetin S5a/PSMD4 Antibody [L2F5] PSMD11 Antibody [L2N1] PSMB5 Antibody [F16L3] Ubiquitin (linkage-specific K27) Antibody [J11K4] S5a/PSMD4 Antibody [K9M17] RA-190 PSMB6 Antibody [P14M13] Laminin Receptor Antibody [L4P5] MG-115 KSQ-4279 (USP1-IN-1) Proteasome 20S LMP7 Antibody [N6D20]

Chemical Information, Storage & Stability

Molecular Weight	517.12	Formula	C₂₀H₂₃BCl₂N₂O₉	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1239908-20-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (193.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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.
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.67mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.650mg/ml (1.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	20S proteasome β5 site ^[1] (Cell-free assay) 0.93 nM(Ki) 20S proteasome β5 site ^[1] (Cell-free assay) 3.4 nM 20S proteasome β1 site ^[1] (Cell-free assay) 31 nM 20S proteasome β2 site ^[1] (Cell-free assay) 3500 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/20160034/ [2] https://pubmed.ncbi.nlm.nih.gov/21903769/ [3] https://www.sciencedirect.com/science/article/pii/B9780124171503000272 [4] https://patents.google.com/patent/WO2016165677A1/en?oq=WO+2016165677

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05882279	Completed	Multiple Myeloma	Takeda	June 1 2023	--
NCT03422874	Withdrawn	Neoplasms\|Lymphoma	Dartmouth-Hitchcock Medical Center	August 2016	Phase 1
NCT02582359	Completed	Acute Myeloid Leukemia	Massachusetts General Hospital\|Millennium Pharmaceuticals Inc.	January 2016	Phase 1

Tech Support

Handling Instructions

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