Home MAPK MNK inhibitor - Wnt/beta-catenin activator - Apoptosis related activator CGP 57380 For research use only.

CGP 57380

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. CGP 57380 upregulates β-catenin and potentiates radiation-induced apoptosis.

CGP 57380 Chemical Structure

CGP 57380 Chemical Structure

CAS: 522629-08-9

Selleck's CGP 57380 has been cited by 6 Publications

1 Customer Review

Purity & Quality Control

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

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Cell Data

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 25800647
Click to View More Cell Line Experimental Data

Biological Activity

Description 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. CGP 57380 upregulates β-catenin and potentiates radiation-induced apoptosis.
Targets
MNK1 [1]
(Cell-free assay)
2.2 μM
In vitro
In vitro CGP57380 inhibits phosphorylation of eIF4E in cellular assays with 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]
In Vivo
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]

Chemical Information & Solubility

Molecular Weight 244.23 Formula

C11H9FN6
CAS No. 522629-08-9 SDF Download CGP 57380 SDF
Smiles C1=CC(=CC=C1NC2=C3C(=NC=NC3=NN2)N)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 48 mg/mL ( (196.53 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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