CGP 57380
Based on 3 publication(s) in Google Scholar
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
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- Purity: 98.71%
- CAS No.: 522629-08-9
- 화학식: C11H9FN6
- 분자량:244.23
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) CGP 57380
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WB
Biological Activity
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MNK1 2.2 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
10.21 μM
Compound: CGP-57380
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Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay
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[PMID: 30115493] |
| HEK293 | IC50 |
1600 nM
Compound: CGP57380
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Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
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[PMID: 30530193] |
| HEK293 | IC50 |
870 nM
Compound: CGP57380
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Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis
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[PMID: 30530193] |
| HL-60 | GI50 |
7.26 μM
Compound: CGP57380
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Antiproliferative activity against human HL-60 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
Antiproliferative activity against human HL-60 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
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[PMID: 34515481] |
| K562 | GI50 |
28.84 μM
Compound: CGP57380
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Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
Antiproliferative activity against human K562 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
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[PMID: 34515481] |
| MOLM-13 | GI50 |
8.81 μM
Compound: CGP57380
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Cytotoxicity against human MOLM13 cells assessed as growth inhibition at 72 hrs by resazurin assay
Cytotoxicity against human MOLM13 cells assessed as growth inhibition at 72 hrs by resazurin assay
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[PMID: 26408454] |
| MOLM-13 | GI50 |
9.88 μM
Compound: CGP57380
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Antiproliferative activity against human MOLM13 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
Antiproliferative activity against human MOLM13 cells assessed as reduction of cell viability incubated for 72 hrs by trypan blue staining based cell counting analysis
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[PMID: 34515481] |
| MOLM-13 | IC50 |
8.24 μM
Compound: CGP-57380
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Antiproliferative activity against human MOLM13 cells after 96 hrs by MTT assay
Antiproliferative activity against human MOLM13 cells after 96 hrs by MTT assay
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[PMID: 30115493] |
| MV4-11 | GI50 |
4.88 μM
Compound: CGP57380
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Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay
Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay
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[PMID: 25800647] |
| MV4-11 | GI50 |
6.89 μM
Compound: CGP57380
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Cytotoxicity against human MV4-11 cells assessed as growth inhibition at 72 hrs by resazurin assay
Cytotoxicity against human MV4-11 cells assessed as growth inhibition at 72 hrs by resazurin assay
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[PMID: 26408454] |
| THP-1 | IC50 |
11.68 μM
Compound: CGP-57380
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Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay
Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay
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[PMID: 30115493] |
CGP57380 inhibits phosphorylation of eIF4E in cellular assays with an IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells[1]. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy[2]. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs)[3]. CGP57380 prevents the serial replating function of BC progenitors[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 522629-08-9
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Appearance Solid
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분자량 244.23
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화학식 C11H9FN6
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Color Light brown to brown
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SMILES
NC1=NC=NC2=C1C(NC3=CC=C(F)C=C3)N=N2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
Proteomic screening identifies RPLp2 as a specific regulator for the translation of coronavirus. [Abstract]2023 Mar 1:230:123191. PMID: 36632964
CGP 57380 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2023 Mar 1:230:123191. [Abstract]
Decreasing the level of p-eIF4E by CGP57380 (0, 2, 20, 50 µM; 24 h) and eFT508 (0, 2, 10 µM; 24 h) result in a dose-dependent decrease in RPLp2, in Vero cells (infected with PEDV).
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Cell Rep
circPRKAA1 activates a Ku80/Ku70/SREBP-1 axis driving de novo fatty acid synthesis in cancer cells. [Abstract]2022 Nov 22;41(8):111707. PMID: 36417875 -
Viruses
The Natural Compound Homoharringtonine Presents Broad Antiviral Activity In Vitro and In Vivo. [Abstract]2018 Nov 1;10(11). pii: E601. PMID: 30388805
용액&용해도
DMSO : ≥ 100 mg/mL (409.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" 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: ≥ 2.5 mg/mL (10.24 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.24 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.
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.
Protocol
Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CD34+ cells (5×105) or GMPs (1×105) are resuspended in 25 μL 1% FBS/PBS solution and injected into the right femur of 8- to 10-wk-old sublethally irradiated (200 cGy) female mice (n=5 mice per group). Mice injected with 1% FBS/PBS solution serve as a sham control for each experiment. Beginning at 4 wk posttransplantation, mice are monitored for engraftment of human cells by flow cytometry. At 6 wk after transplantation, engrafted mice are treated with vehicle alone, dasatinib (5 mg/kg/d) by gavage, or CGP57380 (40 mg/kg/d) intraperitoneally for 3 wk (n=5 mice per group). At the end of treatment, mice are euthanized, and CD45+ cells are isolated from BM and spleen by using anti-human CD45-specific immunomagnetic microbeads. An aliquot of 1×105 human CD45+ cells is seeded into methylcellulose for the colony forming cell (CFC) assay, and colonies are enumerated after 2 wk. All of the remaining human cells from each primary transplant recipient are then transplanted by intrafemoral injection into secondary recipients, and human engraftment is monitored at 2-wk intervals beginning at 4 wk. At the end of 16 wk, all mice are euthanized. Engraftment in BM and blood is assessed by flow cytometry, and BCR-ABL1 transcripts are detected by RT-PCR.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (282 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Knauf U, et al. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol. 2001 Aug;21(16):5500-11. [Content Brief]
[2]. Ishida M, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res. 2003 Dec 12;93(12):1218-24. Epub 2003 Nov 6 [Content Brief]
[3]. Chrestensen CA, et al. Loss of MNK function sensitizes fibroblasts to serum-withdrawal induced apoptosis. Genes Cells. 2007 Oct;12(10):1133-40. [Content Brief]
[4]. Lim S, et al. Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307 [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, 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 | 4.0945 mL | 20.4723 mL | 40.9445 mL | 102.3613 mL |
| 5 mM | 0.8189 mL | 4.0945 mL | 8.1889 mL | 20.4723 mL | |
| 10 mM | 0.4094 mL | 2.0472 mL | 4.0945 mL | 10.2361 mL | |
| 15 mM | 0.2730 mL | 1.3648 mL | 2.7296 mL | 6.8241 mL | |
| 20 mM | 0.2047 mL | 1.0236 mL | 2.0472 mL | 5.1181 mL | |
| 25 mM | 0.1638 mL | 0.8189 mL | 1.6378 mL | 4.0945 mL | |
| 30 mM | 0.1365 mL | 0.6824 mL | 1.3648 mL | 3.4120 mL | |
| 40 mM | 0.1024 mL | 0.5118 mL | 1.0236 mL | 2.5590 mL | |
| 50 mM | 0.0819 mL | 0.4094 mL | 0.8189 mL | 2.0472 mL | |
| 60 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7060 mL | |
| 80 mM | 0.0512 mL | 0.2559 mL | 0.5118 mL | 1.2795 mL | |
| 100 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0236 mL |
CGP 57380 Related Classifications
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