40 CHF CHF 40.00
AG-CR1-3670-M0011 mgCHF 40.00
AG-CR1-3670-M0055 mgCHF 160.00
AG-CR1-3670-M02525 mgCHF 480.00
|Purity Chemicals||≥98% (HPLC)|
|Solubility||Soluble in DMSO (20mg/ml), ethanol (10mg/ml) or DMF (20mg/ml). Poorly soluble in aqueous buffers.|
|Identity||Determined by 1H-NMR.|
|Other Product Data||
Note: Stock solutions are stable for at least 1 month when stored at -20°C.
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Handling Advice||Keep cool and dry.|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Potent selective and reversible proteasome inhibitor (all proteolytic subunits).
- Targets the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50=3.4nM). Cross-reacts and inhibits the trypsin-like β2 subunit (IC50=3.5μM) and the caspase-like/peptidyl-glutamyl peptide-hydrolyzing (PGPH) β1 subunit (IC50=0.03μM).
- Anticancer compound effective in cell-based assays, in xenografts and against multiple myeloma in vivo.
- In vitro, induces cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma.
- Biologically active form of the prodrug MLN9708 (Prod. No. AG-CR1-3671).
- Exhibits improved pharmacodynamics and antitumor activity compared to bortezomib (Prod. No. AG-CR1-3602) in various B cell lymphoma models, due to a greater tumor to blood ratio of proteasome inhibition that ultimately translates into improved tumor pharmacodynamic response and antitumor activity in several tumor xenograft models.
- Evaluation of the proteasome inhibitor MLN9708 in preclinical models of human cancer: E. Kupperman, et al.; Cancer Res. 70, 1970 (2010)
- In vitro and in vivo selective antitumor activity of a novel orally bioavailable proteasome inhibitor MLN9708 against multiple myeloma cells: D. Chauhan, et al.; Clin. Cancer Res. 17, 5311 (2011)
- Antitumor activity of the investigational proteasome inhibitor MLN9708 in mouse models of B-cell and plasma cell malignancies: E.C. Lee, et al.; Clin. Cancer Res. 17, 7313 (2011)
- Investigational agent MLN9708/2238 targets tumor-suppressor miR33b in MM cells: Z. Tian, et al.; Blood 120, 3958 (2012)
- MLN2238, a proteasome inhibitor, induces caspase-dependent cell death, cell cycle arrest, and potentiates the cytotoxic activity of chemotherapy agents in rituximab-chemotherapy-sensitive or rituximab-chemotherapy-resistant B-cell lymphoma preclinical models: J.J. Gu, et al.; Anticancer Drugs 24, 1030 (2013)
- Preclinical activity of the oral proteasome inhibitor MLN9708 in Myeloma bone disease: A. Garcia-Gomez, et al.; Clin. Cancer Res. 20, 1542 (2014)
- The investigational agent MLN2238 induces apoptosis and is cytotoxic to CLL cells in vitro, as a single agent and in combination with other drugs: A. Paulus, et al.; Br. J. Haematol. 165, 78 (2014)
- An evidence-based review of ixazomib citrate and its potential in the treatment of newly diagnosed multiple myeloma: M. Offidani, et al.; Onco. Targets Ther. 7, 1793 (2014)
- The investigational proteasome inhibitor ixazomib for the treatment of multiple myeloma: P.G. Richardson, et al.; Future Oncol. 11, 1153 (2015)
- Comparison of antiproliferative and apoptotic effects of a novel proteasome inhibitor MLN2238 with bortezomib on K562 chronic myeloid leukemia cells: S. Engur, et al.; Immunopharmacol. Immunotoxicol. 38, 87 (2016)
- Proteasomal Inhibition by Ixazomib Induces CHK1 and MYC-Dependent Cell Death in T-cell and Hodgkin Lymphoma: D. Ravi, et al.; Cancer Res. 76, 3319 (2016)
- The potential of ixazomib, a second-generation proteasome inhibitor, in the treatment of multiple myeloma: J. Brayer & R. Baz; Ther. Adv. Hematol. 8, 209 (2017) (Review)