Syk Inhibitor IV, BAY 61-3606 HCl CAS: 732983-37-8
MF: C20H18N6O3•HCl
MW: 426.86
An imidazopyrimidine inhibitor of Syk and Syk-mediated functions.

Syk Inhibitor IV, BAY 61-3606 HCl (CAS 732983-37-8)

Syk Inhibitor IV, BAY 61-3606 HCl | CAS 732983-37-8 is rated 5.0 out of 5 by 1.
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Synonym: BAY 61-3606; 2-(7-(3,4-Dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino)-nicotinamide HCl
Application: An imidazopyrimidine inhibitor of Syk and Syk-mediated functions
CAS Number: 732983-37-8
Purity: ≥97%
Molecular Weight: 426.86
Molecular Formula: C20H18N6O3•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Syk Inhibitor IV, BAY 61-3606 (BAY 61-3606) is a cell-permeable imidazopyrimidine compound that acts as a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki = 7.5 nM) with no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src. BAY 61-3606 has been shown to inhibit Syk-mediated cellular functions such as inhibition of high glucose-tyrosine phosphorylation of I κ B α and p65 nuclear translocation. In mast cells BAY 61-3606 has inhibited cytokine synthesis, lipid mediation and degranulation. In addition, monocyte and eosinophil activation by B cells and Fc receptors were suppressed by BAY 61-3606.


References

1. Yamamoto, N., et al. 2003. J. Pharm. Exp. Ther. 306:1174-1181. PMID: 12766258
2. Yang, W.S., et al. 2008. Am. J. Physiol. Renal Physiol. 294: F1065-F1075. PMID: 18353872

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml), water (20 mg/ml), and methanol.
Storage :
Store at 4° C
IC50 :
Syk tyrosine kinase activity: IC50 = 10 nM
Ki Data :
Syk tyrosine kinase activity: Ki= 7.5 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
52949496
MDL Number :
MFCD18641826
SMILES :
C1=C(C=CC(=C1OC)OC)C3=CC2=NC=C[N]2C(=N3)NC4=NC=CC=C4C(N)=O.Cl

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Certificate of Analysis

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Syk Inhibitor IV, BAY 61-3606 HCl  Product Citations

See how others have used Syk Inhibitor IV, BAY 61-3606 HCl. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 18 total

PMID: # 28949404  Unsal, D.|Kacan, M.|Temiz-Resitoglu, M.|Guden, DS.|Korkmaz, B.|Sari, AN.|Buharalioglu, CK.|Yildirim-Yaroglu, H.|Tamer-Gumus, L.|Tunctan, B.|Malik, KU.|Sahan-Firat, S.| et al. 2018. Clin. Exp. Pharmacol. Physiol. 45: 155-165.

PMID: # 30104977  Ji, N.|Pan, S.|Shao, C.|Chen, Y.|Zhang, Z.|Wang, R.|Qiu, Y.|Jin, M.|Kong, D.| et al. 2018. Front Pharmacol. 9: 824.

PMID: # 29901140  Qiao, Y. et al. 2018. Mol Med Rep. 18: 1995-2008.

PMID: # 26619766  Vandenbriele, C. et al. 2016. Platelets. 27: 365-72.

PMID: # 26456627  Li, X.|Kwon, O.|Kim, DY.|Taketomi, Y.|Murakami, M.|Chang, HW.| et al. 2016. Allergy. 71: 198-209.

PMID: # 25543269  Kremlitzka, M. et al. 2015. Cellular and molecular life sciences : CMLS. 72: 2223-36.

PMID: # 25917838  Li, X. et al. 2015. Journal of ethnopharmacology. 169: 138-44.

PMID: # 26032420  Callaway, JB. et al. 2015. The Journal of biological chemistry. 290: 17306-20.

PMID: # 24612525  Correale, J. et al. 2014. Journal of neuroimmunology. 269: 76-86.

PMID: # 25484046  Swisher, JF. et al. 2014. mAbs. 6: 1377-84.

Citations 1 to 10 of 18 total
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Rated 5 out of 5 by from Bhagwat Bhagwat, SS. (PubMed 18568424) tested the efficacy of Syk Inhibitor IV (BAY 61-3606 HCl) against other inhibitors. Found that the efficacy of BAY 61-3606, at a dose of 30 mg/kg, b.i.d., in suppressing the accumulation of eosinophils in BAL fluid was similar to that of 0.3 mg/kg po, b.i.d., of dexamethasone. The less than adequate pharmacokinetic profile of BAY 61-3606 (low AUC and fast elimination half-life) contributed to the need for the high dose. -SCBT Publication Review
Date published: 2015-03-11
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