WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406177
CAS#: 732983-37-8 (free base)
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.
MedKoo Cat#: 406177
Name: BAY 61-3606
CAS#: 732983-37-8 (free base)
Chemical Formula: C20H18N6O3
Exact Mass: 390.14404
Molecular Weight: 390.4
Elemental 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
Appearance: white 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
The following data is based on the product molecular weight 390.4 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Mitra R, Bhagavatula ID, Gope R. BAY 61-3606, CDKi, and sodium butyrate treatments alter gene expression in human vestibular schwannomas and cause cell death in vitro. Ecancermedicalscience. 2012;6:285. doi: 10.3332/ecancer.2012.285. Epub 2012 Dec 20. PubMed PMID: 23304241; PubMed Central PMCID: PMC3530378.
2: Scheib JL, Sullivan CS, Carter BD. Jedi-1 and MEGF10 signal engulfment of apoptotic neurons through the tyrosine kinase Syk. J Neurosci. 2012 Sep 19;32(38):13022-31. PubMed PMID: 22993420; PubMed Central 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 a genotype-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 kinase mediates high glucose-induced transforming growth factor-β1 up-regulation in proximal tubular epithelial cells. Exp Cell Res. 2012 Sep 10;318(15):1867-76. doi: 10.1016/j.yexcr.2012.05.016. Epub 2012 May 31. PubMed PMID: 22659134.
5: Robak T, Robak E. Tyrosine kinase inhibitors as potential drugs for B-cell lymphoid malignancies and autoimmune disorders. Expert Opin Investig 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 species in human platelets occurs via Syk-dependent and Syk-independent pathways. 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. Spleen tyrosine kinase mediates BEAS-2B cell migration and proliferation and human rhinovirus-induced expression of vascular endothelial growth factor 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, Lippert E, Roche S, Mahon FX, Pasquet JM. Quantitative phosphoproteomics revealed interplay between Syk and Lyn in the resistance to nilotinib in chronic 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 the anti-allergic activity of Syk inhibitors with optimized Syk siRNAs in FcepsilonRI-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 tyrosine phosphorylation of IkappaBalpha in human glomerular endothelial cells: involvement of Syk tyrosine kinase. Am J Physiol Renal Physiol. 2008 May;294(5):F1065-75. doi: 10.1152/ajprenal.00381.2007. Epub 2008 Mar 19. PubMed PMID: 18353872.
648903-57-5 (BAY 61-3606 2HCl)
732983-37-8 (BAY 61-3606 free)