R406 Inhibitor CAS No. 841290-81-1

Cat. No.	Name	Size	Price
KI0211	R406	2 mg	$192
	R406	5 mg	$299.2
	R406	10 mg	$475.2
	R406	50 mg	$1531.2
	R406	200 mg	$4347.2

Chemical Characteristic

Product Name	R406
CAS No.	841290-81-1
Molecular Weight	628.63
Formula	C₂₈H₂₉FN₆O₈S
Chemical Name	6-(5-fluoro-2-(3,4,5-trimethoxyphenylamino)pyrimidin-4-ylamino)-2,2-dimethyl-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one benzenesulfonate
Smiles	O1c2c(NC(=O)C1(C)C)nc(cc2)Nc1nc(ncc1F)Nc1cc(c(c(c1)OC)OC)OC c1(ccccc1)S(=O)(=O)O
Chemical Structure

Biological activities

R406 is an ATP-competitive inhibitor of spleen tyrosine kinase (Syk) kinase with an IC50 of 41 nM. R406 inhibits ATP binding with a K_{i of 30 nM. R406 inhibits all other kinases tested at 5- to 100-fold less potency than Syk by phosphorylation of target proteins. After Syk, Flt3 autophosphorylation is most potently inhibited by R406 at approximately 5-fold less potency than Syk activity. R406 is potent inhibitor of immunoglobulin E (IgE) - and IgG-mediated activation of Fc receptor signaling with an EC50 of 56 nM. R406 exhibits antagonistic activity with an IC50 estimated to be 93 nM. ^[1] R406 inhibits phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. Furthermore, R406 blocks Syk-dependent FcR-mediated activation of monocytes/ macrophages and neutrophils and BCR-mediated activation of B lymphocytes. ^[1] R406 inhibits BCR-derived prosurvival signals. R406 induces CLL cell apoptosis in NLC cocultures. R406 blocks CCL3 and CCL4 secretion by CLL cells in response to BCR triggering and blocks BCR downstream signaling in CLL cells. R406 also blocks the intracellular calcium flux after anti-IgM stimulation. Treatment with R406 effectively blocks calcium mobilization in response to BCR stimulation. R406 inhibits proliferation of Syk-transformed pre-B cells, and induces apoptosis in non-Hodgkin lymphoma (NHL) and CLL cells. R406 abrogates the BCR-dependent up-regulation of important adhesion and costimulatory molecules, such as CD54, CD62L, CD44, CD40, CD80, and CD86. ^[2] In mice, administration of R406 reduces vascular leakage and edema in the Arthus reaction elicited by immune complexes. R406 also shows efficacy in inhibiting paw inflammation in two antibody-induced arthritis mouse models. ^[1]}

Protocols

A 10 mM stock solution of R406, stored in aliquots at -80°C, is diluted in DMSO. ^[1]

References

[1] Braselmann S, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006, 319(3): 998-1008. [2] Quiroga MP, et al. B-cell antigen receptor signaling enhances chronic lymphocytic leukemia cell migration and survival: specific targeting with a novel spleen tyrosine kinase inhibitor, R406. Blood. 2009, 114(5): 1029-1037.

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