Chemical Structure : R406 free base
CAS No.: 841290-80-0
Catalog No.: PC-42815Not For Human Use, Lab Use Only.
R406 (Tamatinib) free base is a potent, specific and orally available Syk kinase inhibitor with Ic50 of 41 nM, inhibits anti-IgE-mediated CHMC degranulation with EC50 of 56 nM.
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R406 (Tamatinib) free base is a potent, specific and orally available Syk kinase inhibitor with Ic50 of 41 nM, inhibits anti-IgE-mediated CHMC degranulation with EC50 of 56 nM.
R406 displays 5- to 100-fold selectivity over a panel of 90 kinases, no activity against Lyn kinase.
R406 does not inhibit phosphorylation of Syk tyrosine 352 but inhibited the phosphorylation of LAT tyrosine 191, inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF.
R406 reduces immune complex-mediated inflammation in arthritis models and is orally active.
M.Wt | 470.4536 | |
Formula | C22H23FN6O5 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
2H-Pyrido[3,2-b]-1,4-oxazin-3(4H)-one, 6-[[5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl]amino]-2,2-dimethyl- |
1. Braselmann S, et al. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.
2. Cha HS, et al. J Pharmacol Exp Ther. 2006 May;317(2):571-8.
3. Matsubara S, et al. Am J Respir Crit Care Med. 2006 Jan 1;173(1):56-63.
4. Pine PR, et al. Clin Immunol. 2007 Sep;124(3):244-57.
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