1. Cell Cycle/DNA Damage
  2. p97
  3. CB-5083

CB-5083 

Cat. No.: HY-12861 Purity: 99.95%
Handling Instructions

CB-5083 is a potent, selective and orally bioavailable p97 inhibitor with an IC50 value of 11 nM.

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

CB-5083 Chemical Structure

CB-5083 Chemical Structure

CAS No. : 1542705-92-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE CB-5083

    CB-5083 purchased from MCE. Usage Cited in: Leukemia. 2019 Jul;33(7):1675-1686.

    Jeko-1 and Z138C cells are exposed to the indicated concentrations of CB-5083 and ACY-1215 in the presence or absence of the autophagy inhibitor chloroquine for 6 h and LC3B-II and p62 expression is assessed by immunoblot analysis.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CB-5083 is a potent, selective and orally bioavailable p97 inhibitor with an IC50 value of 11 nM.

    IC50 & Target

    IC50: 11 nM (p97)[1]

    In Vitro

    Treatment of tumor cells with CB-5083 leads to significant accumulation of markers associated with inhibition of ubiquitin−proteasome system and endoplasmic reticulum-associated degradation functions, which induces irresolvable proteotoxic stress and cell death[1]

    In Vivo

    In tumor bearing mice, oral administration of CB-5083 causes rapid accumulation of markers of the unfolded protein response and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. CB-5083 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors[1].

    Clinical Trial
    Molecular Weight

    413.47

    Formula

    C₂₄H₂₃N₅O₂

    CAS No.

    1542705-92-9

    SMILES

    O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (241.86 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4186 mL 12.0928 mL 24.1856 mL
    5 mM 0.4837 mL 2.4186 mL 4.8371 mL
    10 mM 0.2419 mL 1.2093 mL 2.4186 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 (6.05 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

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

    The ATPase assay is performed to determine the IC50 value. compounds (CB-5083) are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 μM. The assay is done in a 384-well plate with each row as a single dilution

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

    Cell Assay
    [1]

    A549 and other tumor cell lines are cultured according to ATCC guidelines. Cells are cultured in black or white, clear-bottomed, tissue culture-treated 384-well plates. Cells are treated with 10-point dose titration of the compound (CB-5083) in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability[1].

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

    Animal Administration
    [1]

    Mice: Tumor-bearing mice are used to evaluate pharmacokinetics and pharmacodynamics effect and antitumor activity. Both molecules (CB-5083 and compoud 69) are administered orally as a suspension in 0.5% methylcellulose aqueous suspensions at the fixed dose strength of 150 mg/kg; plasma and tumor samples at multiple time points (2, 6, 16, and 24 h) are harvested for pharmacokinetics and pharmacodynamics analysis[1].

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

    References

    Purity: 99.95%

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    Inquiry Information

    Product Name:
    CB-5083
    Cat. No.:
    HY-12861
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