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    Bortezomib (PS-341; Velcade)
    Bortezomib (PS-341; Velcade)

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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 #: V0684
    CAS #: 179324-69-7Purity ≥98%

    Description: Bortezomib (foremrly also known as PS-341; trade names name Velcade among others), a dipeptide boronic acid derivative, is cell-permeable, reversible, potent and highly selective inhibitor of 20S proteasome with potential antitumor activity. It inhibits 20S proteasome with a Ki of 0.6 nM in a cell-free assay. The ubiquitin-proteasome pathway plays a critical role in the regulated degradation of proteins involved in cell cycle control and tumor growth. Dysregulating the degradation of such proteins should have profound effects on tumor growth and cause cells to undergo apoptosis. As a potent 20S proteasome inhibitor, bortezomib has potential antineoplastic activity and was approved in 2003 in the U.S. and Europe for the treatment relapsed multiple myeloma and mantle cell lymphoma. Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. In vivo, bortezomib delays tumor growth and enhances the cytotoxic effects of radiation and chemotherapy. 

    References: Cancer Res. 1999;59(11):2615-22; Cancer Cell Int. 2005;5(1):18; Cancer Res. 2002;62(17):4996-5000.

    Related CAS: 205393-22-2 (Bortezomib-pinanediol)

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    Molecular Weight (MW)384.24
    FormulaC19H25BN4O4
    CAS No.179324-69-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 76 mg/mL (197.8 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+ddH2O: 5 mg/mL
    SynonymsPS-341; PS341; NSC 681239; MLN-341; PS 341; LDP 341; LDP-341; LDP341; MLN341; MLN 341. Brand name: VELCADE; NSC681239; NSC-681239
    Chemical Name((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid 
    SMILES CodeCC(C)C[[email protected]@H](B(O)O)NC([[email protected]@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O


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    In Vitro

    In vitro activity: Bortezomib is a boronic acid dipeptide that s a highly selective, reversible inhibitor of the 26S proteasome which primarily functions in the degradation of mis-folded proteins and is essential for the regulation of the cell cycle. Exposure to Bortezomib has been shown to stabilize p21, p27, and p53, as well as the proapoptotic Bid and Bax proteins, caveolin-1, and inhibitor κB-α, which prevents activation of nuclear factor κB-induced cell survival pathways. Bortezomib also promotes the activation of the proapoptotic c-Jun-NH2 terminal kinase, as well as the endoplasmic reticulum stress response. Alteration of the levels of these cellular proteins leads to inhibition of proliferation, migration, and promotion of apoptosis of cancer cells. Bortezomib is shown to penetrate into cells and inhibit proteasome-mediated intracellular proteolysis of long-lived proteins with a concentration that inhibits 50% of the proteolysis of ∼0.1 μM. The average growth inhibition of 50% value for Bortezomib across the entire panel of 60 cancer cell lines derived from multiple human tumors from the US National Cancer Institute (NCI) is 7 nM. Treatment of PC-3 cells with Bortezomib (100 nM) for 8 h results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1. Bortezomib kills PC-3 cells at 24 and 48 hr with IC50 of 100 and 20 nM, respectively. Bortezomib induces nuclear condensation at 16–24 hr after treatment. Bortezomib treatment leads to PARP cleavage in a time-dependent manner with concentrations as low as 100 nM being effective at 24 hr.


    Kinase Assay: a typical kinetic run, 2.00 mL of assay buffer (20 mM HEPES, 0.5 mM EDTA, 0.035% SDS, pH 7.8) and Suc-Leu-Leu-Val-Tyr-AMC in DMSO are added to a 3 mL fluorescence cuvette, and the cuvette is placed in the jacketed cell holder of a fluorescence spectrophotometer. Reaction temperature is maintained at 37℃ by a circulating water bath. After the reaction solution has reached thermal equilibrium (5 minutes), 1 μL−10 μL of the stock enzyme solution is added to the cuvette. Reaction progress is monitored by the increase in fluorescence emission at 440 nm (λex= 380 nm) that accompanies cleavage of AMC from peptide-AMC substrates.


    Cell Assay: The inhibitory effect of Bortezomib on cell growth is assessed by measuring MTT dye absorbance of the cells. Cells (Human multiple myeloma cells line U266) from 48-hour cultures are pulsed with 10 μL of 5 mg/mL MTT to each well for the last 4 hour of 48-hour cultures, followed by 100 μL of isopropanol containing 0.04 N HCl. Absorbance is measured at 570 nm using a spectrophotometer.

    In VivoThe anticancer effects of bortezomib as a single agent have been demonstrated in xenograft models of multiple myeloma, adult T-cell leukemia, lung, breast, prostate, pancreatic, head and neck, and colon cancer, and in melanoma. Oral bortezomib 1.0 mg/ kg daily for 18 days causes tumor growth delays, as well as a decrease in the number of metastases in the Lewis lung cancer model. Bortezomib at a single dose of up to 5 mg/kg significantly decreased the surviving fraction of breast tumor cells. Bortezomib 1.0 mg/kg administrated weekly for 4 weeks reduces tumor growth by 60% in murine xenograft models of prostate cancer. 1.0 mg/kg Bortezomib administration for 4 weeks results in a 72% or 84% reduction in pancreatic cancer murine xenografts growth, as well as an increase in tumor cell apoptosis. 1.0 mg/kg Bortezomib treatment results in significant inhibition of human plasmacytoma xenograft growth, increase in tumor cells apoptosis and overall survival, and a decrease in tumor angiogenesis.
    Animal modelHuman plasmacytoma xenografts RPMI 8226
    Formulation & DosageDissolved in Saline; 1 mg/kg; i.v. injection
    ReferencesCancer Res. 1999 Jun 1;59(11):2615-22; Cancer Cell Int. 2005 Jun 1;5(1):18; Cancer Res. 2002 Sep 1;62(17):4996-5000.



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

     

    Bortezomib (PS-341)

    PS-341 induces apoptosis in PC-3 cells. Cancer Res.1999 Jun 1;59(11):2615-22.
     

    Bortezomib (PS-341)

    Effect on PC-3 tumor growth in mice after four weekly i.v. injections of vehicle or PS-341 (a) or after direct injection of PS-341 or vehicle (b) into the PC-3 tumor on 4 consecutive days. Cancer Res. 1999 Jun 1;59(11):2615-22.
     

    Bortezomib (PS-341)

    Effect on 20S proteasome activity in murine WBCs (a) and in PC-3 tumors (b), 1.0 h after i.v. dosing of PS-341. Cancer Res. 1999 Jun 1;59(11):2615-22.

    Bortezomib (PS-341)

    Bortezomib (PS-341)

    Bortezomib (PS-341)


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