CGP-57380


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

Description

Cas:522629-08-9

Product Information:

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 CGP57380 suppressed eIF4E phosphorylation, proliferation, and colony formation whereas concomitant treatment with CGP57380 and the mTOR inhibitor rapamycin accentuated growth inhibition and cell-cycle arrest.

 

Chemical Formula: C11H9FN6

 

Exact Mass: 244.0873

 

Molecular Weight: 244.2334

 

Elemental Analysis: C, 54.10; H, 3.71; F, 7.78; N, 34.41

 

Synonym:

 

CGP-57380

CGP57380

CGP 57380

 

Chemical Name:

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

 

InChi Key:

UQPMANVRZYYQMD-UHFFFAOYSA-N

 

InChi Code:

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)

 

Smiles Code:

NC1=C2C(NN=C2NC3=CC=C(F)C=C3)=NC=N1

 

 

Technical Data:

 

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). CGP57380 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. Martínez A, Sesé M, Losa JH, Robichaud N, Sonenberg N, Aasen T, Ramón Y Cajal S. Phosphorylation of eIF4E Confers Resistance to Cellular Stress and DNA-Damaging Agents through an Interaction with 4E-T: A Rationale for Novel Therapeutic Approaches. PLoS One. 2015 Apr 29;10(4):e0123352. doi: 10.1371/journal.pone.0123352. eCollection 2015. PubMed PMID: 25923732; PubMed Central PMCID: PMC4414544.

 

  1. 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.

 

  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.

 

  1. 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.

 

  1. Allard EK, Grujic M, Fisone G, Kristensson K. Prion formation correlates with activation of translation-regulating protein 4E-BP and neuronal transcription factor Elk1. Neurobiol Dis. 2013 Oct;58:116-22. doi: 10.1016/j.nbd.2013.05.014. Epub 2013 Jun 3. PubMed PMID: 23742760.

 

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

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