CB-5339
Based on 2 publication(s) in Google Scholar
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.58%
- CAS. Nr.: 1863952-15-1
- Formel: C24H24N6O
- Molecular Weight:412.49
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Lösungsmittel & Löslichkeit
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- Verweise
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Publications Citing Use of MedChemExpress (MCE) CB-5339
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.7 μM
Compound: CB-5339
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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
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[PMID: 36228523] |
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.
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Cell Line:MV4-11 AML cell line
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Concentration:0,0.2,0.4,0.8,1.6 μM
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Incubation Time:24-48 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MLL-AF9-driven patient-derived xenograft (PDX) AML model in C57BL/6 male mice[2]
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Dosage:90 mg/kg
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Administration:oral gavage (p.o.)
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Result:Decreased bone marrow leukemic infiltration and circulating leukemic cells.
Prolonged mice survival.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1863952-15-1
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Appearance Solid
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Molecular Weight 412.49
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Formel C24H24N6O
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Color Off-white to yellow
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SMILES
O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(CCCN5)C5=N3)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
CRISPR screens identify the ATPase VCP as a druggable therapeutic vulnerability in cholangiocarcinoma. [Abstract]2025 Sep 30;122(39):e2519568122. PMID: 40991439 -
FASEB J
FAT1 Enhances the Sensitivity of Non-Small Cell Lung Cancer to VCP Inhibitors by Regulating the Activation of the Endoplasmic Reticulum Stress Pathway. [Abstract]2025 May 15;39(9):e70585. PMID: 40293794
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.06 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. David Wustrow, et al. FUSED PYRIMIDINES AS INHIBITORS OF p97 COMPLEX. WO2015109285A1.
[2]. Roux B, et.al. Targeting acute myeloid leukemia dependency on VCP-mediated DNA repair through a selective second-generation small-molecule inhibitor. Sci Transl Med. 2021 Mar 31;13(587):eabg1168. [Content Brief]
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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