CGP 57380

Name: CGP 57380
Brand: MedChemExpress
SKU: HY-10520
Rating: 5.0 (5 reviews)

Cat. No.: HY-10520 Purity: 98.71%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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.

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

CGP 57380 Chemical Structure

CAS No. : 522629-08-9

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 5 publication(s) in Google Scholar

4 Publications Citing Use of MCE CGP 57380

: CGP 57380 purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2023 Jan 9;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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MNK1 MNK2 MNK

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

MNK1

2.2 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	10.21 μM Compound: CGP-57380	Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay	[PMID: 30115493]
HEK293	IC₅₀	1600 nM Compound: CGP57380	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	[PMID: 30530193]
HEK293	IC₅₀	870 nM Compound: CGP57380	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	[PMID: 30530193]
HL-60	GI₅₀	7.26 μM Compound: CGP57380	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	[PMID: 34515481]
K562	GI₅₀	28.84 μM Compound: CGP57380	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	[PMID: 34515481]
MOLM-13	IC₅₀	8.24 μM Compound: CGP-57380	Antiproliferative activity against human MOLM13 cells after 96 hrs by MTT assay Antiproliferative activity against human MOLM13 cells after 96 hrs by MTT assay	[PMID: 30115493]
MOLM-13	GI₅₀	8.81 μM Compound: CGP57380	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	[PMID: 26408454]
MOLM-13	GI₅₀	9.88 μM Compound: CGP57380	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	[PMID: 34515481]
MV4-11	GI₅₀	4.88 μM Compound: CGP57380	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	[PMID: 25800647]
MV4-11	GI₅₀	6.89 μM Compound: CGP57380	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	[PMID: 26408454]
THP-1	IC₅₀	11.68 μM Compound: CGP-57380	Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay	[PMID: 30115493]

In Vitro

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.

In Vivo

CGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs^[4].

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

Molecular Weight

244.23

Formula

C₁₁H₉FN₆

CAS No.

522629-08-9

Appearance

Solid

Color

Light brown to brown

SMILES

NC1=NC=NC2=C1C(NC3=CC=C(F)C=C3)N=N2

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 (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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	4.0945 mL	20.4723 mL	40.9445 mL
5 mM	0.8189 mL	4.0945 mL	8.1889 mL
10 mM	0.4094 mL	2.0472 mL	4.0945 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 (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.
Protocol 2

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.

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: 98.71%

Select Batch:

Data Sheet (282 KB) SDS (392 KB)

COA (251 KB) LCMS (96 KB)

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]

Kinase Assay ^[1]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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

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

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:

CGP 57380522629-08-9CGP57380CGP-57380MNKApoptosisMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseInhibitorinhibitorinhibit

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CGP 57380

Customer Review

CGP 57380 Related Antibodies

4 Publications Citing Use of MCE CGP 57380

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

CGP 57380 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

CGP 57380 Related Classifications

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