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CB-5083

Name: CB-5083
Brand: TargetMol
SKU: T6796
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: CB5083, CB 5083) Copy Product Info

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Synonyms: CB5083, CB 5083

Catalog No. T6796 Copy Product Info

Purity: 99.92%

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CB-5083 is an effective, selective, orally available p97 AAA ATPase inhibitor with an IC50 of 11 nM. CB-5083 exhibits broad-spectrum antitumor activity. CB-5083 can be used in studies of protein homeostasis disruption, endoplasmic reticulum stress, and tumor drug resistance.

Cas No. 1542705-92-9

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Pack Size	Price	USA Stock	Global Stock
1 mg	$38	In Stock	In Stock
2 mg	$54	In Stock	In Stock
5 mg	$89	In Stock	In Stock
10 mg	$139	In Stock	In Stock
25 mg	$313	In Stock	In Stock
50 mg	$493	In Stock	In Stock
100 mg	$723	In Stock	In Stock
500 mg	$1,520	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$98	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.92%

Color:White

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COA HNMR HPLC

Product Introduction

Bioactivity

Description	CB-5083 is an effective, selective, orally available p97 AAA ATPase inhibitor with an IC50 of 11 nM. CB-5083 exhibits broad-spectrum antitumor activity. CB-5083 can be used in studies of protein homeostasis disruption, endoplasmic reticulum stress, and tumor drug resistance.
Targets & IC50	p97 AAA ATPase:11 nM
In vitro	Methods: Patient-derived myoblasts (p.R155H) were treated with CB-5083 (75, 100, 150 nM) for 5 days. Western blot analysis was performed to detect MFN2, p62, LC3, TFEB, and VCP protein levels. Results: CB-5083 induced significant upregulation of MFN2 levels, along with marked increases in autophagy markers p62 and the LC3-II/I ratio. No significant changes were observed in TFEB or total VCP levels. [1] Methods: Eleven osteosarcoma cell lines (U2OS, HOS, SJSA-1, etc.) and human osteoblasts (hFOB1.19) were treated with CB-5083 at concentrations ranging from 0 to 8 μM for 72 hours. Cell viability was assessed using the MTT assay, and the half-maximal inhibitory concentration (IC₅₀) was calculated. Results: CB-5083 exhibited a dose-dependent inhibitory effect on osteosarcoma cells with an IC₅₀ range of 0.3286–1.032 μM.[2]
In vivo	Methods: Homozygous VCPR 155H/R155H mice (2 months old) received oral gavage of CB-5083 at 15 mg/kg/day once daily for 5 months. Results: CB-5083 was well tolerated with normal body weight. Serum AST and CK showed a decreasing trend, with no hepatotoxicity observed. Rotarod performance did not significantly deteriorate. [1] Methods: Nude mice were subcutaneously implanted with SJSA-1 cells. Upon reaching a tumor volume of 100 mm³, oral gavage administration of CB-5083 (100 mg/kg/day) was initiated once daily for 30 days. Results: Tumor volume in the CB-5083-treated group was significantly smaller than the control group starting from day 15. At the endpoint, the mean tumor weight was significantly higher in the control group (823 mg) than in the CB-5083 group (416 mg).[2]
Synonyms	CB5083, CB 5083
Kinase Assay	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	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)

Chemical Properties

Molecular Weight	413.47
Formula	C₂₄H₂₃N₅O₂
Cas No.	1542705-92-9
Smiles	Cc1cc2c(cccc2n1-c1nc2CCOCc2c(NCc2ccccc2)n1)C(N)=O
Relative Density.	1.37 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 11 mg/mL (26.6 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 247.5 mg/mL (598.59 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 6 mg/mL (14.51 mM), Solution.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4186 mL	12.0928 mL	24.1856 mL	120.9278 mL
5 mM	0.4837 mL	2.4186 mL	4.8371 mL	24.1856 mL
10 mM	0.2419 mL	1.2093 mL	2.4186 mL	12.0928 mL
20 mM	0.1209 mL	0.6046 mL	1.2093 mL	6.0464 mL

DMSO

	1mg	5mg	10mg	50mg
50 mM	0.0484 mL	0.2419 mL	0.4837 mL	2.4186 mL
100 mM	0.0242 mL	0.1209 mL	0.2419 mL	1.2093 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.