1. Metabolic Enzyme/Protease
    Autophagy
    Apoptosis
  2. Proteasome
    Autophagy
    Apoptosis
  3. Carfilzomib

Carfilzomib (Synonyms: PR-171)

Cat. No.: HY-10455 Purity: 99.96%
Handling Instructions

Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

For research use only. We do not sell to patients.

Carfilzomib Chemical Structure

Carfilzomib Chemical Structure

CAS No. : 868540-17-4

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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Carfilzomib purchased from MCE. Usage Cited in: J Agric Food Chem. 2017 Jun 7;65(22):4384-4394.

    Resveratrol activates the HSF1 signaling pathway. J-Lat A2 cells are treated with various concentrations of Resveratrol or Carfilzomib (50 nM) for 48 h. Then the cells are lysed and Ser320 phosphorylated HSF1 and total HSF1 are detected by Western blot with corresponding antibodies.

    Carfilzomib purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.

    J-Lat 10.6 cells are treated with DMSO, PR-957 (150 nM) or Carfilzomib (40 nM) alone with or without the HSF1 inhibitor KRIBB11 (1.25 µM) for 48 h. Then the cells are lysed, and Ser320 phosphorylated HSF1, total HSF1 and p24 are detected by Western blot with the corresponding antibodies.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Carfilzomib is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

    IC50 & Target

    IC50: 5 nM (Proteasome)

    In Vitro

    Carfilzomib displays preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM and above and little or no effect on the PGPH and T-L activities at doses up to 100 nM. Carfilzomib decreases the viability of ANBL-6, RPMI 8226 cells, U266 and KAS-6/1 cells with an IC50 less than 5 nM. Carfilzomib overcome Dex resistance, in that MM1.R cells reveals an IC50 of 15.2 nM, less than the value of 29.3 nM for parental MM1.S cells[1]. Co-treatment with carfilzomib and HDACIs leads to synergistic induction of cell death in various mantle cell lymphoma lines and primary mantle cell lymphoma cells. Combined treatment with carfilzomib or ONX0912 with vorinostat in HF-4B and Granta cells sharply increases caspase activation, PARP cleavage, JNK activation, MnSOD2 induction, and DNA damage[2].

    In Vivo

    Carfilzomib (2.0 mg/kg, i.v.) in conbination with 70 mg/kg vorinostat virtually abrogates tumor growth in Granta-luciferace cell xenograft flank model. Combined treatment results in a pronounced reduction in bioluminescence compared to animals treated with single agents or controls with minimal toxicity[2].

    Clinical Trial
    Molecular Weight

    719.91

    Formula

    C₄₀H₅₇N₅O₇

    CAS No.

    868540-17-4

    SMILES

    C[[email protected]@]1(C([[email protected]](CC(C)C)NC([[email protected]@H](NC([[email protected]](CC(C)C)NC([[email protected]@H](NC(CN2CCOCC2)=O)CCC3=CC=CC=C3)=O)=O)CC4=CC=CC=C4)=O)=O)OC1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years

    *The compound is unstable in solutions, freshly prepared is recommended.

    Solvent & Solubility
    In Vitro: 

    DMF : ≥ 100 mg/mL (138.91 mM)

    DMSO : 50 mg/mL (69.45 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3891 mL 6.9453 mL 13.8906 mL
    5 mM 0.2778 mL 1.3891 mL 2.7781 mL
    10 mM 0.1389 mL 0.6945 mL 1.3891 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    WST-1 is used to determine the effects of proteasome inhibitors on cell proliferation according to the manufacturer's protocol. The inhibition of proliferation is calculated in relation to parallel control cells that receive vehicle alone and tabulated in KaleidaGraph 3.0.1 or Excel 2000. A linear spline function is used to interpolate the median inhibitory concentration (IC50) using XLfit 4 software. The degree of resistance (DOR) is calculated using the formula: DOR=IC50(resistant cells)/IC50(sensitive cells).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Animal studies are performed utilizing Beige-nude-XID mice. 10×106 Granta514 cells are pelleted, washed twice with 1X PBS, injected subcutaneously into the right flank. Once the tumors are visible, 5 to 6 mice are treated with carfilzomib±vorinostat and progress of tumor growth or regression is monitored. Stock vorinostat and carfilzomib is dissolved in DMSO and 10% sulfobutylether betacyclodextrin in 10 mM citrate buffer pH respectively. They are stored in −80°C in small aliquots and diluted before injection.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.96%

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    Keywords:

    CarfilzomibPR-171PR171PR 171ProteasomeAutophagyApoptosisInhibitorinhibitorinhibit

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    Cat. No.:
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