CB-5083
For research use only.
Catalog No.S8101
18 publications
CAS No. 1542705-92-9
CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
3 Customer Reviews
-
LN229 GBM cell lysates were immunoblotted with antibodies recognizing specific focal adhesion proteins. Note the decreased levels of Cas, paxillin, and FAK tyrosine phosphorylation in cells treated with CB-5083. In addition, CB-5083 treatment leads to decreased levels of total PTP-PEST expression, but Vcp protein expression levels are not impacted.
Cancer Res, 2018, 78(14):3809-3822. CB-5083 purchased from Selleck.
-
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.
-
Cycloheximide (CHX) chase experiments in the presence of the unrelated competitive p97 inhibitor CB-5083 (5 μm) or DMSO alone. Cells were lysed at indicated time points after CHX addition and lysates subjected to Western blotting. Tubulin was probed as loading control. UT = untreated.
Mol Cell Proteomics, 2018, 17(7):1295-1307. CB-5083 purchased from Selleck.
Purity & Quality Control
Choose Selective ATPase Inhibitors
Biological Activity
| Description | CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1. | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
|||||||||||||||||||||||
| 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] |
|||||||||||||||||||||||
| Cell Data |
|
|||||||||||||||||||||||
| Assay |
|
|||||||||||||||||||||||
| 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] |
- Collapse
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] |
- Collapse
|
| Animal Research:[1] |
- Collapse
|
Solubility (25°C)
| In vitro | DMSO | 82 mg/mL (198.32 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | '13 mg/mL warmed | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 0.5% CMC Na+5% Tween 80 For best results, use promptly after mixing. |
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 |
| Smiles | CC1=CC2=C(C=CC=C2N1C3=NC4=C(COCC4)C(=N3)NCC5=CC=CC=C5)C(=O)N |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*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).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT02243917 | Terminated | Drug: CB-5083 | Advanced Solid Tumors | Cleave Biosciences Inc. | October 11 2014 | Phase 1 |
| NCT02223598 | Terminated | Drug: CB-5083|Drug: Dexamethasone | Lymphoid Hematological Malignancies|Relapsed and Refractory Multiple Myeloma | Cleave Biosciences Inc. | August 25 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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
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.
