CB-5083

Name: CB-5083
Brand: MedChemExpress
SKU: HY-12861
Rating: 5.0 (23 reviews)

Cat. No.: HY-12861 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

CB-5083 Chemical Structure

CAS No. : 1542705-92-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 121	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 121	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 610	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 980	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 23 publication(s) in Google Scholar

22 Publications Citing Use of MCE CB-5083

: CB-5083 purchased from MedChemExpress. Usage Cited in: Leukemia. 2019 Jul;33(7):1675-1686. [Abstract]; Jeko-1 and Z138C cells are exposed to the indicated concentrations of CB-5083 and ACY-1215 in the presence or absence of the autophagy inhibitor chloroquine for 6 h and LC3B-II and p62 expression is assessed by immunoblot analysis.

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Biological Activity
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References
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Description

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.

In Vivo

CB-5083 (75 mg/kg; oral administration; qd; for 2 weeks) shows antitumor activity in an HCT 116 tumor xenograft model^[1].
CB-5083 exhibits terminal elimination half-life (T_1/2=2.56 h), moderate oral bioavailability (mouse 41%) and C_max (mouse 7.95 μM) following oral administration (25 mg/kg) in female nude mice^[1].
CB-5083 exhibits terminal elimination half-life (T_1/2=2.83 h) due to high plasma clearance (5.9 mL/min/kg respectively) combined with large volumes of distribution (418 mL/kg respectively) following intravenous administration (3.0 mg/kg) in female nude mice^[1].
CB-5083 has good metabolic stability with a 102 min T_1/2 in a mouse liver microsomal stability study and a 172 min T_1/2 in a hepatocyte stability study^[1].

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

Animal Model:	Nu/Nu nude female mice bearing established human tumor xenografts derived from HCT 116 colon^[1]
Dosage:	75 mg/kg
Administration:	Administered orally using every day (qd) dosing, for 2 weeks.
Result:	Showed more profound antitumor activity.

Clinical Trial

Molecular Weight

413.47

Formula

C₂₄H₂₃N₅O₂

CAS No.

1542705-92-9

Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

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

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4186 mL	12.0928 mL	24.1856 mL	60.4639 mL
	5 mM	0.4837 mL	2.4186 mL	4.8371 mL	12.0928 mL
	10 mM	0.2419 mL	1.2093 mL	2.4186 mL	6.0464 mL
	15 mM	0.1612 mL	0.8062 mL	1.6124 mL	4.0309 mL
	20 mM	0.1209 mL	0.6046 mL	1.2093 mL	3.0232 mL
	25 mM	0.0967 mL	0.4837 mL	0.9674 mL	2.4186 mL
	30 mM	0.0806 mL	0.4031 mL	0.8062 mL	2.0155 mL
	40 mM	0.0605 mL	0.3023 mL	0.6046 mL	1.5116 mL
	50 mM	0.0484 mL	0.2419 mL	0.4837 mL	1.2093 mL
	60 mM	0.0403 mL	0.2015 mL	0.4031 mL	1.0077 mL
	80 mM	0.0302 mL	0.1512 mL	0.3023 mL	0.7558 mL
	100 mM	0.0242 mL	0.1209 mL	0.2419 mL	0.6046 mL

CB-5083 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CB-50831542705-92-9CB5083CB 5083p97VCPCdc48multiplemyelomasolidtumorsAAAATPaseInhibitorinhibitorinhibit

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CB-5083

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22 Publications Citing Use of MCE CB-5083

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