2. Cell Cycle/DNA Damage
  3. p97
  4. CB-5339

CB-5339 is an oral activity potent p97 inhibitor with an IC50 <30 nM. CB-5339 can be used for leukemia research. CB-5339 extracted from WO2015109285A1 compound FF07.

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

CB-5339 Chemical Structure

CB-5339 Chemical Structure

CAS No. : 1863952-15-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 242 In-stock
Solution
10 mM * 1 mL in DMSO USD 242 In-stock
Solid
5 mg USD 220 In-stock
10 mg USD 360 In-stock
25 mg USD 720 In-stock
50 mg USD 1260 In-stock
100 mg USD 2200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

CB-5339 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CB-5339 is an oral activity potent p97 inhibitor with an IC50 <30 nM. CB-5339 can be used for leukemia research[1]. CB-5339 extracted from WO2015109285A1 compound FF07.

Cellular Effect
Cell Line Type Value Description References
HCT-116 IC50
0.7 μM
Compound: CB-5339
Anti-proliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo luminescent assay
Anti-proliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CellTiter-Glo luminescent assay
[PMID: 36228523]
In Vitro

CB-5339( 0-1.6 μM; 24-48 hours) induces polyubiquitin protein accumulation and activates of the unfolded protein response (UPR) in AML cells[2].

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

CB-5339 Related Antibodies

Western Blot Analysis[2]

Cell Line: MV4-11 AML cell line
Concentration: 0,0.2,0.4,0.8,1.6 μM
Incubation Time: 24-48 hours
Result: Induced dose-dependent polyubiquitin protein accumulation at concentrations ≥ 0.4 μM.
Induced the ER stress marker GRP78 accumulated at concentrations ≥ 0.4 μM.
Induced spliced XBP-1 and ATF-4 accumulated after treatment with CB-5339 at concentrations ≥ 1.6 μM and 0.8 μM respectively arguing for a concentration-dependent increase in proteotoxic stress.
In Vivo

CB-5339 (90 mg/kg for p.o.) decreases bone marrow leukemic infiltration and prolongs mice survival in MLL-AF9-driven patient-derived xenograft (PDX) AML mouse model[2].

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

Animal Model: MLL-AF9-driven patient-derived xenograft (PDX) AML model in C57BL/6 male mice[2]
Dosage: 90 mg/kg
Administration: oral gavage (p.o.)
Result: Decreased bone marrow leukemic infiltration and circulating leukemic cells.
Prolonged mice survival.
Clinical Trial
Molecular Weight

412.49

Formula

C24H24N6O
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(CCCN5)C5=N3)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (242.43 mM; ultrasonic and warming and heat to 80°C; 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 2.4243 mL 12.1215 mL 24.2430 mL
5 mM 0.4849 mL 2.4243 mL 4.8486 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 mg/mL (5.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.58%

SDS (251 KB)

COA (255 KB) HNMR (141 KB) RP-HPLC (169 KB) LCMS (112 KB)

Handling Instructions (2659 KB)
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4243 mL 12.1215 mL 24.2430 mL 60.6075 mL
5 mM 0.4849 mL 2.4243 mL 4.8486 mL 12.1215 mL
10 mM 0.2424 mL 1.2122 mL 2.4243 mL 6.0608 mL
15 mM 0.1616 mL 0.8081 mL 1.6162 mL 4.0405 mL
20 mM 0.1212 mL 0.6061 mL 1.2122 mL 3.0304 mL
25 mM 0.0970 mL 0.4849 mL 0.9697 mL 2.4243 mL
30 mM 0.0808 mL 0.4041 mL 0.8081 mL 2.0203 mL
40 mM 0.0606 mL 0.3030 mL 0.6061 mL 1.5152 mL
50 mM 0.0485 mL 0.2424 mL 0.4849 mL 1.2122 mL
60 mM 0.0404 mL 0.2020 mL 0.4041 mL 1.0101 mL
80 mM 0.0303 mL 0.1515 mL 0.3030 mL 0.7576 mL
100 mM 0.0242 mL 0.1212 mL 0.2424 mL 0.6061 mL
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CB-5339 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-53391863952-15-1CB5339CB 5339p97VCPCdc48p97 inhibitorMV4-11 AML cellsubiquitinUPRxenograf modelleukemiaInhibitorinhibitorinhibit

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