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Chemical Structure| 1239908-20-3 Chemical Structure| 1239908-20-3

Structure of Ixazomib citrate
CAS No.: 1239908-20-3

Chemical Structure| 1239908-20-3

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Ixazomib citrate is the citrate form of ixazomib which is an inhibitor of chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 of 3.4 nM.

Synonyms: MLN9708; Ninlaro

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Product Details of Ixazomib citrate

CAS No. :1239908-20-3
Formula : C20H23BCl2N2O9
M.W : 517.12
SMILES Code : O=C1C(CC(O)=O)(CC(O)=O)OB([C@@H](NC(CNC(C2=CC(Cl)=CC=C2Cl)=O)=O)CC(C)C)O1
Synonyms :
MLN9708; Ninlaro
MDL No. :MFCD29767859
InChI Key :MBOMYENWWXQSNW-AWEZNQCLSA-N
Pubchem ID :56844015

Safety of Ixazomib citrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
U266 13.66 µM 48 h Inhibited cell proliferation PMC10489073
MM.1S 1, 2, 4 µM 48 h Induced cell apoptosis and cell cycle arrest PMC10489073
HCC PDXOs 0.1 μM 48 h To assess the effect of Ixazomib on the viability of HCC PDXOs, results showed that Ixazomib significantly reduced cell viability. PMC9377092
HCC PDXOs 1 μM 48 h To evaluate the cytotoxic effect of Ixazomib on HCC PDXOs, results showed that Ixazomib significantly reduced cell viability. PMC9377092
L428 25 nM 24 h Global transcriptome analyses of L428 cells treated with ixazomib showed significant gene changes with a 1.2 fold-change for 423 genes PMC5315412
L540 25 nM 24 h Global transcriptome analyses of L540 cells treated with ixazomib showed significant gene changes with a 1.2 fold-change for 4765 genes PMC5315412
Jurkat 25 nM 24 h Global transcriptome analyses of Jurkat cells treated with ixazomib showed significant gene changes with a 1.2 fold-change for 508 genes PMC5315412

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice HCC PDX model Oral gavage 7 mg/kg Three times a week, continuous treatment To evaluate the tumor inhibitory effect of Ixazomib in combination with Dinaciclib on HCC PDX models, results showed that the combination treatment significantly inhibited tumor growth. PMC9377092
Mice Multiple myeloma xenograft models Orally 3 mg/kg Twice weekly The antitumor efficacy of M3258, bortezomib, and ixazomib was compared in vivo. In the U266B1 multiple myeloma model, ixazomib induced prolonged complete tumor regression. PMC9398180
Mice HF/HC/BS diet model Oral 20 mg/kg Single dose, 6 hours To evaluate the effect of ixazomib on LXRα ubiquitination, results showed that ixazomib treatment significantly reduced the ubiquitination level of LXRα. PMC4947007
Mice IL6Myc mouse model Intravenous injection 7 mg/kg Twice weekly for 24 weeks To evaluate the therapeutic response of ixazomib in IL6Myc mouse model of plasma cell tumors, results showed that ixazomib significantly extended the survival of mice. PMC3880444
SCID mice Human lymphoma xenograft models derived from Jurkat and L540 cell lines Intraperitoneal injection 0.36 mg/kg or 0.72 mg/kg Daily for three weeks Investigation of the antitumor activity of ixazomib in Jurkat and L540 xenograft models showed significant tumor growth inhibition and improved survival in mice PMC5315412
NOD.SCID/NCR mice A549 xenograft tumor model Subcutaneous injection 15 mg/kg Daily for 3 weeks To evaluate the inhibitory effect of Ixazomib combined with AKT and SRC inhibitors on the growth of A549 xenograft tumors. The results showed that Ixazomib combined with MK-2206 or Saracatinib significantly reduced tumor growth, and the effect was greatest with the three-drug combination. PMC8642553
Mice H22 pulmonary metastasis tumor model Oral 0.008 mmol/kg Twice weekly for 2 weeks Evaluated anti-metastasis efficacy, significantly reduced the number of pulmonary metastasis nodes PMC10489073
Mice AML xenograft model Oral 8 mg/kg Twice a week for 3 weeks Ixazomib significantly inhibits tumor growth and is associated with suppression of FOXM1. PMC6129129

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00963820 Multiple Myeloma PHASE1 COMPLETED 2025-01-14 Mayo Clinic- Scottsdale, Scott... More >>sdale, Arizona, 85259, United States|James R. Berenson, MD, Inc, West Hollywood, California, 90069, United States|University of Chicago, Chicago, Illinois, 60637, United States|Mayo Clinic, Rochester, Minnesota, 55905, United States|Weill-Cornell Medical College, New York, New York, 10011, United States|Fred Hutchinson Cancer Research Center, Seattle, Washington, 98109, United States Less <<
NCT02168101 Multiple Myeloma PHASE2 COMPLETED 2019-02-01 Colorado Blood Cancer Institut... More >>e, Denver, Colorado, 80218, United States|Oncology Hematology Care, Cincinnati, Ohio, 45242, United States|Tennessee Oncology PLLC, Nashville, Tennessee, 37203, United States|Texas Transplant Institute, San Antonio, Texas, 78229, United States Less <<
NCT02169791 Acute Leukemia|Chronic Leukemi... More >>a|Myelodysplastic Syndrome|Lymphomas|Multiple Myeloma Less << PHASE2 COMPLETED 2020-07-28 Northside Hospital, Atlanta, G... More >>eorgia, 30342, United States Less <<
NCT02158975 Lymphoma, T-Cell PHASE2 COMPLETED 2025-11-16 University of Michigan Hospita... More >>l, Ann Arbor, Michigan, 48109, United States Less <<
NCT03965624 Immune Thrombocytopenia|Warm A... More >>utoimmune Hemolytic Anemia Less << PHASE2 WITHDRAWN 2023-09-01 Mahevas, Créteil, 94000, Franc... More >>e Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.67mL

1.93mL

0.97mL

19.34mL

3.87mL

1.93mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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