Catalog No. size PriceQuantity
M6497-2 2mg solid $113
M6497-10 10mg solid $431


CGP-57380 is a selective inhibitor of MAP kinase-interacting kinase 1 (MNK1) in vitro (IC50 = 2.2 μM). MNK1 overexpression was confirmed in both primary GBMs and glioma cell lines. Inhibition of MNK1 activity in GBM cells by the small molecule CGP-57380 suppressed eIF4E phosphorylation, proliferation, and colony formation whereas concomitant treatment with CGP-57380 and the mTOR inhibitor rapamycin accentuated growth inhibition and cell-cycle arrest.

Product information

CAS Number: 522629-08-9

Molecular Weight: 244.23

Formula: C11H9FN6


CGP 57380



Chemical Name: N3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidine-3,4-diamine

Smiles: NC1N=CN=C2NN=C(NC3C=CC(F)=CC=3)C2=1


InChi: InChI=1S/C11H9FN6/c12-6-1-3-7(4-2-6)16-11-8-9(13)14-5-15-10(8)17-18-11/h1-5H,(H4,13,14,15,16,17,18)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

CGP-57380 inhibits phosphorylation of eIF4E in cellular assays with IC50 of about 3 μM. CGP-57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. CGP-57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. CGP-57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). CGP-57380 prevents the serial replating function of BC progenitors.

In Vivo:

CGP-57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs.


  1. Grzmil M, Huber RM, Hess D, Frank S, Hynx D, Moncayo G, Klein D, Merlo A, Hemmings BA. MNK1 pathway activity maintains protein synthesis in rapalog-treated gliomas. J Clin Invest. 2014 Feb;124(2):742-54. doi: 10.1172/JCI70198. Epub 2014 Jan 9. PubMed PMID: 24401275; PubMed Central PMCID: PMC3904612.
  2. Dumoulin MC, Aton SJ, Watson AJ, Renouard L, Coleman T, Frank MG. Extracellular signal-regulated kinase (ERK) activity during sleep consolidates cortical plasticity in vivo. Cereb Cortex. 2015 Feb;25(2):507-15. doi: 10.1093/cercor/bht250. Epub 2013 Sep 17. PubMed PMID: 24047601; PubMed Central PMCID: PMC4303804.
  3. Diab S, Teo T, Kumarasiri M, Li P, Yu M, Lam F, Basnet SK, Sykes MJ, Albrecht H, Milne R, Wang S. Discovery of 5-(2-(phenylamino)pyrimidin-4-yl)thiazol-2(3H)-one derivatives as potent Mnk2 inhibitors: synthesis, SAR analysis and biological evaluation. ChemMedChem. 2014 May;9(5):962-72. doi: 10.1002/cmdc.201300552. Epub 2014 Feb 12. PubMed PMID: 24677692.

Products are for research use only. Not for human use.

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