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CB-5083
Catalog No.S8101
For research use only.
CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
CAS No. 1542705-92-9
Selleck's CB-5083 has been cited by 30 publications
Purity & Quality Control
Choose Selective ATPase Inhibitors
Related Compound Libraries
Other ATPase Products
Biological Activity
| Description | CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| 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] |
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| Cell Data |
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| Assay |
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| 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 (from reference)
| Kinase Assay:[1] |
|
|---|---|
| Cell Research:[1] |
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| Animal Research:[1] |
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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 to the product individually and in order |
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 | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| 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)
mg/kg
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 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.
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 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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.
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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.
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Products are for research use only. Not for human use. We do not sell to patients.
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