Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

CB-5083 [1542705-92-9]

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Referência HY-12861-1ml

Tamanho : 10mM/1mL

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Description

CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC₅₀ of 11 nM^[1].

IC₅₀ & Target

IC50: 11 nM (p97)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.49 μM Compound: 71	Inhibition of p97 ATPase in human A549 cells assessed as reduction in p62 protein incubated for 6 hrs by immunofluorescence assay Inhibition of p97 ATPase in human A549 cells assessed as reduction in p62 protein incubated for 6 hrs by immunofluorescence assay	[PMID: 26565666]
A549	IC₅₀	0.68 μM Compound: 71	Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by Celltiter-Glo assay Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by Celltiter-Glo assay	[PMID: 26565666]
A549	IC₅₀	0.68 μM Compound: 71	Inhibition of p97 ATPase in human A549 cells assessed as accumulation of K48 poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay Inhibition of p97 ATPase in human A549 cells assessed as accumulation of K48 poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay	[PMID: 26565666]
A549	IC₅₀	1.03 μM Compound: 71	Inhibition of p97 ATPase in human A549 cells assessed as accumulation of CHOP poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay Inhibition of p97 ATPase in human A549 cells assessed as accumulation of CHOP poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay	[PMID: 26565666]
A549	IC₅₀	1.3 μM Compound: CB-5083	Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 assay	[PMID: 30606672]
A549	IC₅₀	1.7 μM Compound: CB-5083	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 33831696]
RPMI-8226	IC₅₀	0.8 μM Compound: CB-5083	Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 33831696]

In Vitro

CB-5083 shows cell killing potency with IC₅₀s of 0.68, 0.68, 1.03, and 0.49 μM for lung carcinoma A549 CTG, A549 K48, A549 CHOP, and A549 p62, respectively^[1].

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (241.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (24.19 mM); Clear solution; Need ultrasonic

Pureté et documentation

Purity: 99.90%

Fiche technique (279 KB) SDS (393 KB)

COA (255 KB) HNMR (190 KB) LCMS (121 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Zhou HJ, et al. Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083). J Med Chem. 2015 Dec 24;58(24):9480-97. [Content Brief]

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Referência HY-12861-1ml

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

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