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    OPROZOMIB (ONX-0912)
    OPROZOMIB (ONX-0912)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0691
    CAS #: 935888-69-0Purity ≥98%

    Description: Oprozomib (formerly known as ONX 0912 and PR 047) is a novel, potent, and orally bioavailable small molecule inhibitor for chymotrypsin-like (CT)-L activity of 20S proteasome β5/LMP7 with potential antitumor activity. It inhibits 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.  Oprozomib exhibited high antitumor activity in vivo in multiple human tumor xenograft and mouse syngeneic models.

    References: J Med Chem. 2009 May 14;52(9):3028-38; Blood. 2010 Dec 2;116(23):4906-15. 

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    Molecular Weight (MW)532.61
    FormulaC25H32N4O7S
    CAS No.935888-69-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (187.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES Code O=C(C1=CN=C(C)S1)N[[email protected]@H](COC)C(N[[email protected]@H](COC)C(N[[email protected]@H](CC2=CC=CC=C2)C([[email protected]]3(C)OC3) =O)=O)=O
    SynonymsONX-0912; ONX0912; PR047; ONX 0912;PR-047; PR 047. 

    Chemical Name: N-((S)-3-methoxy-1-(((S)-3-methoxy-1-(((S)-1-((R)-2-methyloxiran-2-yl)-1-oxo-3-phenylpropan-2-yl)amino)-1-oxopropan-2-yl)amino)-1-oxopropan-2-yl)-2-methylthiazole-5-carboxamide

    InChi Key: SWZXEVABPLUDIO-WSZYKNRRSA-N

    InChi Code: InChI=1S/C25H32N4O7S/c1-15-26-11-20(37-15)24(33)29-19(13-35-4)23(32)28-18(12-34-3)22(31)27-17(21(30)25(2)14-36-25)10-16-8-6-5-7-9-16/h5-9,11,17-19H,10,12-14H2,1-4H3,(H,27,31)(H,28,32)(H,29,33)/t17-,18-,19-,25+/m0/s1

    SMILES Code: O=C(C1=CN=C(C)S1)N[[email protected]@H](COC)C(N[[email protected]@H](COC)C(N[[email protected]@H](CC2=CC=CC=C2)C([[email protected]]3(C)OC3)=O)=O)=O


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    In Vitro

    In vitro activity: The anti-MM activity of Oprozomib is associated with activation of caspase-8, caspase-9, caspase-3, and PARP, as well as inhibition of migration of MM cells and angiogenesis.


    Kinase Assay: Samples (lysed cells or tissue homogenates) are treated for 1 h at room temperature with the biotinylated active site probe PR-584 (5-15 μM). Samples are denatured by addition of SDS (0.9% final) and heating to 100 °C for 5 min. The denatured samples are transferred to a 96-well or 384-well filter plat, mixed with streptavidin-sepharose beads (2.5-5 μL packed beads/well), and incubated for 1 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer (PBS, 1% bovine serum albumin, 0.1% Tween-20) by vacuum filtration. The beads are incubated overnight at 4 °C on a plate shaker with the following antibodies recognizing the six catalytic subunits diluted into ELISA buffer: β5, β1, and β2 diluted 1:3000, LMP7 and LMP2 diluted 1:5000, and MECL-1 diluted 1:1000. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and incubated with HRP-conjugated secondary antibody diluted 1:5000 in ELISA buffer and incubated 2 h at room temperature on a plate shaker. The beads are washed 5 times with 100-200 μL /well of ELISA buffer and developed for chemiluminsecence signal using the supersignal ELISA pico substrate following the manufacturer's instructions. Luminescence is measured on a plate reader and converted to ng of proteasome or μg/ml of lysate by comparison with 20S proteasome or untreated cell lysate standard curves. For proteasome inhibitor studies, active site probe binding values are expressed as the percent of binding relative to DMSO treated cells. 


    Cell Assay:In trypan blue exclusion assays, ONX 0912 exhibited IC50 values ranging from 58.9 to185.7 nmol/L in 8 different HNSCC cell lines. In the 4 HNSCC cell lines (UMSCC-1, UMSCC-22B, 1483, and UMSCC-1) examined, treatment ONX 0912 resulted in processing of caspase-3 to active subunits and cleavage of the caspase substrate PARP.

    In VivoOprozomib is demonstrated an absolute bioavailability of up to 39% in rodents and dogs. It is well tolerated with repeated oral administration at doses resulting in >80% proteasome inhibition in most tissues and elicited an antitumor response in multiple human tumor xenograft and mouse syngeneic models.
    Animal modelNon-Hodgkin’s lymphoma cell line RL xenograft, colorectal tumor cell line CT-26 xenograft
    Formulation & DosageDissolved in 10% (v/v) EtOH and 10% (v/v) PS80 in citrate buffer (pH 3.5); 30 mg/kg; p.o. administration
    References

    J Med Chem. 2009 May 14;52(9):3028-38; Blood. 2010 Dec 2;116(23):4906-15. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    OPROZOMIB (ONX 0912)

    ONX 0912 inhibits growth of xenografted human MM cells in mice. Blood. 2010 Dec 2;116(23):4906-15.

    OPROZOMIB (ONX 0912)

    Effect of ONX 0912 on apoptosis, neovascularization, and ubiquitination in vivo in xenografted MM tumors. Blood. 2010 Dec 2;116(23):4906-15.
     

    OPROZOMIB (ONX 0912)

    OPROZOMIB (ONX 0912)

    Proteasome inhibitor ONX 0912 is structurally distinct from bortezomib and carfilzomib, inhibits proteasome activity in vitro, and triggers MM cell death. Blood. 2010 Dec 2;116(23):4906-15. 

    OPROZOMIB (ONX 0912)

    ONX 0912 inhibits growth of xenografted human MM cells in mice. Blood. 2010 Dec 2;116(23):4906-15. 

    OPROZOMIB (ONX 0912)

    ONX 0912 triggers apoptosis in MM cells, associated with PARP cleavage and caspase activation. Blood. 2010 Dec 2;116(23):4906-15. 


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