CB-5083

Catalog No.S8101

CB-5083 Chemical Structure

Molecular Weight(MW): 413.47

CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.

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USD 547 In stock
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1 Customer Review

  • Incubation with VCP inhibitors results in activation of Unfolded Protein Response (UPR). SKOV3 cells were incubated with (C) 2.5 μM CB-5083 for 0, 1, 3, 6, 12, 24 and 48 h. Whole cell lysates were subjected to Western blot analysis and probed for UPR-related proteins

    Mol Oncol, 2016, 10(10):1559-1574. CB-5083 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
Targets
p97 AAA ATPase [1]
(Cell-free assay)
11 nM
In vitro

In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM. [1]

In vivo In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition. [1]

Protocol

Kinase Assay:[1]
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ATPase assay:

Compounds 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 series with duplicate of each compound concentration point. In 5 μL total volume, 20 nM p97 hexameric enzyme and 20 μM ATP are added to start the reaction. The plate is sealed and incubated at 37 °C for 15 min after mixing thoroughly in an orbital shaker. Compound dilution, ATP and enzymes addition are conducted with automated liquid handling using the Freedom Evo. ADP Glo reagents 1 and 2 are added according to the manufacturer’s protocol. The luminescence is measured by Envision plate reader as the end point of the reaction. The IC50 of each compound is derived by fitting the luminescence values to a four-parameter sigmoidal curve.
Cell Research:[1]
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  • Cell lines: A549 cells
  • Concentrations: ~40.0 μM
  • Incubation Time: 72 h
  • Method: 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 in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability. Luminescence values are fit to a four-parameter sigmoidal curve to determine IC50 concentrations.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Nu/Nu nude female mice bearing human HCT 116 colon tumor xenografts
  • Formulation: Suspended in 0.5% methylcellulose in water
  • Dosages: 75 mg/kg, qd
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (198.32 mM)
Ethanol 13 mg/mL warmed (31.44 mM)
Water Insoluble
In vivo Add solvents individually and in order:
0.5% CMC Na+5% Tween 80
30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 413.47
Formula

C24H23N5O2

CAS No. 1542705-92-9
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02243917 Recruiting Advanced Solid Tumors Cleave Biosciences, Inc. October 2014 Phase 1
NCT02223598 Recruiting Lymphoid Hematological Malignancies|Relapsed and Refractory Multiple Myeloma Cleave Biosciences, Inc. July 2014 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    I am trying to administrate the compound to mice. Does this compound ever dissolve completely?

  • Answer:

    S8101 CB-5083 can be dissolved in 0.5% CMC Na+5% Tween 80 at 30 mg/ml as a suspension for oral gavage.

ATPase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID