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CGP 57380 MNK inhibitor

Name: CGP 57380
Brand: Selleck Chemicals
SKU: S7421
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S7421

CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. This compound upregulates β-catenin and potentiates radiation-induced apoptosis.

Chemical Structure

Molecular Weight: 244.23

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Quality Control

Batch: S742101 DMSO]48 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 98.25%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

98.25

Related Targets	ERK p38 MAPK Raf JNK MEK Ras KRas S6 Kinase MAP4K TAK1
Other MNK Inhibitors	Tomivosertib (eFT-508) SEL201 ETC-206 (AUM 001)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
MV4-11 cells	Growth inhibition assay		72 h		Growth inhibition of human MV4-11 cells after 72 hrs by resazurin assay, GI50=4.88 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (196.53 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (20.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (1.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	244.23	Formula	C₁₁H₉FN₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	522629-08-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=CC=C1NC2=C3C(=NC=NC3=NN2)N)F

Mechanism of Action

Targets/IC₅₀/Ki	MNK1 (Cell-free assay) 2.2 μM
In vitro	CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. This compound causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. It results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. This chemical sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). It prevents the serial replating function of BC progenitors.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11463832/ [2] https://pubmed.ncbi.nlm.nih.gov/14605021/ [3] https://pubmed.ncbi.nlm.nih.gov/17903173/ [4] https://pubmed.ncbi.nlm.nih.gov/23737503/

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Handling Instructions

Tel: +1-832-582-8158 Ext:3

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