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R406

Chemical Structure : R406

CAS No.: 841290-81-1

R406 (R 406;R-406;Tamatinib)

Catalog No.: PC-42880Not For Human Use, Lab Use Only.

R406 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

R406 (Tamatinib) 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.

Physicochemical Properties

M.Wt 628.6287
Formula C28H29FN6O8S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 61 mg/mL

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-, benzenesulfonate (1:1)

References

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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