AdipoGen Life Sciences

Oprozomib [ONX 0912]

As low as CHF 70.00

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AG-CR1-3672-M0011 mgCHF 70.00

AG-CR1-3672-M0055 mgCHF 180.00

Specifications / Handling

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Product Details
Synonyms	O-Methyl-N-[(2-methyl-5-thiazolyl)carbonyl]-L-seryl-O-methyl-N-[(1S)-2-[(2R)-2-methyl-2-oxiranyl]-2-oxo-1-(phenylmethyl)ethyl]-L-serinamide; PR-047
Product Type	Chemical
Properties
Formula	C₂₅H₃₂N₄O₇S
MW	532.6
CAS	935888-69-0
Purity Chemicals	≥98% (HPLC)
Appearance	White solid.
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.
InChi Key	SWZXEVABPLUDIO-WSZYKNRRSA-N
Smiles	O=C([C@]1(CO1)C)[C@H](CC2=CC=CC=C2)NC([C@H](COC)NC([C@H](COC)NC(C3=CN=C(C)S3)=O)=O)=O
Shipping and Handling
Shipping	AMBIENT
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.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Scientific Background Information

Product Description

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.

Product-specific References

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)

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