CX-6258
Based on 4 publication(s) in Google Scholar
CX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.06%
- No. CAS: 1202916-90-2
- Fòrmula: C26H24ClN3O3
- Peso molecular:461.94
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) CX-6258
More
Actividad biológica
IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | CC50 |
>8 μM
Compound: 58; CX-6258
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Cytotoxicity against HEK293T cells
Cytotoxicity against HEK293T cells
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[PMID: 33539089] |
| HeLa | CC50 |
>8 μM
Compound: 58; CX-6258
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Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
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[PMID: 33539089] |
| MV4-11 | IC50 |
>10 μM
Compound: 13
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Inhibition of Flt3 phosphorylation at Y591 in human MV411 cells after 2 hrs by Western blot analysis
Inhibition of Flt3 phosphorylation at Y591 in human MV411 cells after 2 hrs by Western blot analysis
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[PMID: 24900437] |
| PC-3 | IC50 |
452 nM
Compound: 13
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Cytotoxicity against human PC3 cells assessed as viability after 96 hrs
Cytotoxicity against human PC3 cells assessed as viability after 96 hrs
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[PMID: 24900437] |
CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively[1].
CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells[2].
CX-6258 treatment results in a significant reduction in NKX3.1 half-life[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 human AML cells
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Concentration:0.1 μM, 1 μM, 10 μM
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Incubation Time:2 hours
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Result:Caused dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice, MV-4-11 xenograft models[1]
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Dosage:50 mg/kg, 100 mg/kg
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Administration:Oral administration; once daily; over a period of 21 days
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Result:Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.
Chemical Information
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No. CAS 1202916-90-2
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Appearance Solid
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Peso molecular 461.94
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Fòrmula C26H24ClN3O3
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Color Yellow to orange
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SMILES
O=C1NC2=CC=C(Cl)C=C2/C1=C\C3=CC=C(C4=CC=CC(C(N5CCCN(C)CC5)=O)=C4)O3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
PIM1 Attenuates Innate Immunity to Foster Coronavirus Replication through Ubiquitin Ligase β-TrCP-Mediated IFNAR1 Degradation. [Abstract]2025 Jul 6:e03487. PMID: 40619619 -
Inflammopharmacology
Quercetin-loaded exosomes derived from human umbilical cord mesenchymal stem cells alleviate microglia-mediated neuroinflammation via an anti-inflammatory mechanism. [Abstract]2026 May;34(5):3469-3482. PMID: 42014646 -
ACS Med Chem Lett
Serial PNA-Transformer-Based Virtual Screening Identifies Nanomolar DYRK1A Inhibitors for Pancreatic Ductal Adenocarcinoma. [Abstract]2026 Feb 20;17(3):695-703. PMID: 41847637 -
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (108.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.75 mg/mL (5.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
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.
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 20 mg/mL (43.30 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1648 mL | 10.8239 mL | 21.6478 mL | 54.1196 mL |
| 5 mM | 0.4330 mL | 2.1648 mL | 4.3296 mL | 10.8239 mL | |
| 10 mM | 0.2165 mL | 1.0824 mL | 2.1648 mL | 5.4120 mL | |
| 15 mM | 0.1443 mL | 0.7216 mL | 1.4432 mL | 3.6080 mL | |
| 20 mM | 0.1082 mL | 0.5412 mL | 1.0824 mL | 2.7060 mL | |
| 25 mM | 0.0866 mL | 0.4330 mL | 0.8659 mL | 2.1648 mL | |
| 30 mM | 0.0722 mL | 0.3608 mL | 0.7216 mL | 1.8040 mL | |
| 40 mM | 0.0541 mL | 0.2706 mL | 0.5412 mL | 1.3530 mL | |
| 50 mM | 0.0433 mL | 0.2165 mL | 0.4330 mL | 1.0824 mL | |
| 60 mM | 0.0361 mL | 0.1804 mL | 0.3608 mL | 0.9020 mL | |
| 80 mM | 0.0271 mL | 0.1353 mL | 0.2706 mL | 0.6765 mL | |
| 100 mM | 0.0216 mL | 0.1082 mL | 0.2165 mL | 0.5412 mL |
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