Oprozomib [ONX 0912]
60 CHF CHF 60.00
AG-CR1-3672-M0011 mgCHF 60.00
AG-CR1-3672-M0055 mgCHF 145.00
AG-CR1-3672-M02525 mgCHF 435.00
|Purity Chemicals||≥98% (HPLC)|
|Solubility||Soluble in DMSO (20mg/ml) or DMF (10mg/ml). Sparingly soluble in ethanol (1mg/ml). Poorly soluble in aqueous buffers.|
|Identity||Determined by 1H-NMR.|
|Other Product Data||
Note: Warming and sonication may be required when dissolving the compound in the solvent of choice. 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 orally bioavailable irreversible proteasome inhibitor. Analog of Carfilzomib (Prod. No. AG-CR1-3669).
- Targets the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50=36nM) and the β5i subunit [LMP7] of the 20S immunoproteasome (IC50=82nM).
- 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, as well as in bortezomib resistant multiple myeloma cells.
- Shown to have anti-angiogenic activity.
- Has potential applications in certain types of cancer as well as other diseases that require proteasome activity.
- Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047): H.J. Zhou, et al.; J. Med. Chem. 52, 3028 (2009)
- A novel orally active proteasome inhibitor ONX 0912 triggers in vitro and in vivo cytotoxicity in multiple myeloma: D. Chauhan, et al.; Blood 116, 4906 (2010)
- The epoxyketone-based proteasome inhibitors carfilzomib and orally bioavailable oprozomib have anti-resorptive and bone-anabolic activity in addition to anti-myeloma effects: M.A. Hurchla, et al.; Leukemia 27, 430 (2013)
- Carfilzomib and ONX 0912 inhibit cell survival and tumor growth of head and neck cancer and their activities are enhanced by suppression of Mcl-1 or autophagy: Y. Zang, et al.; Clin. Cancer Res. 18, 5639 (2012)
- The next generation proteasome inhibitors carfilzomib and oprozomib activate prosurvival autophagy via induction of the unfolded protein response and ATF4: Y. Zang, et al.; Autophagy 8, 1873 (2012)
- Effect of novel proteasome and immunoproteasome inhibitors on dendritic cell maturation, function, and expression of IκB and NFκB: A.S. Al-Homsi, et al.; Transpl. Immunol. 29, 1 (2013)
- Overview of proteasome inhibitor-based anti-cancer therapies: Perspective on bortezomib and second generation proteasome inhibitors versus future generation inhibitors of ubiquitin-proteasome system: Q.P. Dou & J.A. Zonder; Curr. Cancer Drug Targets 14, 517 (2014)
- Proteasome inhibitors - molecular basis and current perspectives in multiple myeloma: L. Kubiczkova, et al.; J. Cell. Mol. Med. 18, 947 (2014)
- Next-generation proteasome inhibitor oprozomib synergizes with modulators of the unfolded protein response to suppress hepatocellular carcinoma: Y.P. Vandewynckel, et al.; Oncotarget 7, 34988 (2016)
- Second Generation Proteasome Inhibitors in Multiple Myeloma: A. Gozzetti, et al.; Anticancer Agents Med. Chem. 17, 920 (2017)
- Anti-angiogenic and anti-multiple myeloma effects of oprozomib (OPZ) alone and in combination with pomalidomide (Pom) and/or dexamethasone (Dex): E. Sanchez, et al.; Leuk. Res. 57, 45 (2017) (Review)