BAY 61-3606

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WARNING: This product is for research use only, not for human or veterinary use.

Description:BAY 61-3606 is a potent (Ki = 7.5 nM) and selective inhibitor of Syk kinase. BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606.

Price and Availability

BAY 61-3606 , purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406177Name: BAY 61-3606CAS#: 732983-37-8 (free base)Chemical Formula: C20H18N6O3Exact Mass: 390.14404Molecular Weight: 390.4Elemental Analysis: C, 61.53; H, 4.65; N, 21.53; O, 12.29

Synonym:BAY 613606; BAY613606; BAY-613606.

IUPAC/Chemical Name:2-((7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl)amino)nicotinamide

InChi Key:SPMFEULFGGPQLN-UHFFFAOYSA-N

InChi Code:InChI=1S/C20H18N6O3.2ClH/c1-28-15-6-5-12(10-16(15)29-2)14-11-17-22-8-9-26(17)20(24-14)25-19-13(18(21)27)4-3-7-23-19;;/h3-11H,1-2H3,(H2,21,27)(H,23,24,25);2*1H

SMILES Code:O=C(N)C1=C(NC2=NC(C3=CC=C(OC)C(OC)=C3)=CC4=NC=CN24)N=CC=C1.[H]Cl.[H]Cl

Technical Data

Additional Information

  Related: 648903-57-5 (BAY 61-36062HCl) 732983-37-8 (BAY 61-3606free)  

References

1: Mitra R, Bhagavatula ID, Gope R. BAY 61-3606, CDKi,and sodium butyrate treatments alter gene expression in human vestibularschwannomas and cause cell death in vitro. Ecancermedicalscience.2012;6:285. doi: 10.3332/ecancer.2012.285. Epub 2012 Dec 20. PubMedPMID: 23304241; PubMed Central PMCID: PMC3530378.

2: Scheib JL, Sullivan CS, Carter BD. Jedi-1 and MEGF10 signalengulfment of apoptotic neurons through the tyrosine kinase Syk. JNeurosci. 2012 Sep 19;32(38):13022-31. PubMed PMID: 22993420; PubMedCentral PMCID: PMC3464495.

3: Lau KS, Zhang T, Kendall KR, Lauffenburger D, Gray NS, Haigis KM.BAY61-3606 affects the viability of colon cancer cells in agenotype-directed manner. PLoS One. 2012;7(7):e41343. doi:10.1371/journal.pone.0041343. Epub 2012 Jul 18. PubMed PMID: 22815993;PubMed Central PMCID: PMC3399817.

4: Yang WS, Chang JW, Han NJ, Lee SK, Park SK. Spleen tyrosine kinasemediates high glucose-induced transforming growth factor-β1up-regulation in proximal tubular epithelial cells. Exp Cell Res. 2012Sep 10;318(15):1867-76. doi: 10.1016/j.yexcr.2012.05.016. Epub 2012 May31. PubMed PMID: 22659134.

5: Robak T, Robak E. Tyrosine kinase inhibitors as potential drugs forB-cell lymphoid malignancies and autoimmune disorders. Expert OpinInvestig Drugs. 2012 Jul;21(7):921-47. doi:10.1517/13543784.2012.685650. Epub 2012 May 22. Review. PubMed PMID:22612424.

6: Arthur JF, Qiao J, Shen Y, Davis AK, Dunne E, Berndt MC, Gardiner EE,Andrews RK. ITAM receptor-mediated generation of reactive oxygen speciesin human platelets occurs via Syk-dependent and Syk-independentpathways. J Thromb Haemost. 2012 Jun;10(6):1133-41. doi:10.1111/j.1538-7836.2012.04734.x. PubMed PMID: 22489915.

7: Wang X, Mychajlowycz M, Lau C, Gutierrez C, Scott JA, Chow CW. Spleentyrosine kinase mediates BEAS-2B cell migration and proliferation andhuman rhinovirus-induced expression of vascular endothelial growthfactor and interleukin-8. J Pharmacol Exp Ther. 2012 Feb;340(2):277-85.doi: 10.1124/jpet.111.186429. Epub 2011 Oct 26. PubMed PMID: 22031919.

8: Gioia R, Leroy C, Drullion C, Lagarde V, Etienne G, Dulucq S, LippertE, Roche S, Mahon FX, Pasquet JM. Quantitative phosphoproteomicsrevealed interplay between Syk and Lyn in the resistance to nilotinib inchronic myeloid leukemia cells. Blood. 2011 Aug 25;118(8):2211-21. doi:10.1182/blood-2010-10-313692. Epub 2011 Jul 5. PubMed PMID: 21730355.

9: Sanderson MP, Gelling SJ, Rippmann JF, Schnapp A. Comparison of theanti-allergic activity of Syk inhibitors with optimized Syk siRNAs inFcepsilonRI-activated RBL-2H3 basophilic cells. Cell Immunol.2010;262(1):28-34. doi: 10.1016/j.cellimm.2009.12.004. Epub 2009 Dec 14.PubMed PMID: 20053395.

10: Yang WS, Seo JW, Han NJ, Choi J, Lee KU, Ahn H, Lee SK, Park SK.High glucose-induced NF-kappaB activation occurs via tyrosinephosphorylation of IkappaBalpha in human glomerular endothelial cells:involvement of Syk tyrosine kinase. Am J Physiol Renal Physiol. 2008May;294(5):F1065-75. doi: 10.1152/ajprenal.00381.2007. Epub 2008 Mar 19.PubMed PMID: 18353872.