R935788 Inhibitor CAS No. 1025687-58-4

Cat. No.	Name	Size	Price
KI0098	R935788	2 mg	$432
	R935788	5 mg	$600
	R935788	10 mg	$1392
	R935788	50 mg	$4272
	R935788	100 mg	$5920

Chemical Characteristic

Product Name	R935788
Synonyms	R788, Fostamatinib disodium
CAS No.	1025687-58-4
Molecular Weight	624.42
Formula	C₂₃H₂₄FN₆O₉P.₂Na
Chemical Structure

Biological activities

Fostamatinib is the prodrug of R406, a specific ATP-competitive spleen tyrosine kinase (SYK) inhibitor with an IC50 of 41 nM. Fostamatinib is rapidly converted to R406 by human intestinal microsomes, and only low levels of fostamatinib are observed in plasma of human. Fostamatinib has already been successfully tested in rheumatoid arthritis, immune thrombocytopenic purpura, and B-cell lymphomas in both rodent models. The metabolite R406 specifically blocks FcεRI signaling in mast cells and inhibits FcγR and B-cell receptor (BCR) Syk-dependent signaling. ^[1] R406 inhibits ligand-dependent and -independent BCR signaling in TCL1 leukemias in vitro. R406 completely inhibits the anti-IgM induced BCR signal in both cell lines. The prodrug fostamatinib itself effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolongs survival of the treated animals. Fostamatinib treatment after adoptive transfer significantly prevents the outgrowth of these leukemia cells (TCL1-551, TCL1-870). Fostamatinib induces an early and transient mobilization of both normal and malignant B cells, which is subsequently followed by selective inhibition of the growth of the malignant B-cell population. After 16 days of fostamatinib treatment, a significant decrease in the percentage and number of CD5+/B220+ cells is observed in mice, with a further reduction by the last day of treatment. ^[2] Fostamatinib abrogates lipopolysaccharide (LPS) (1 mg/kg)閳ユ悆nduced SYK phosphorylation at the autophosphorylation site Tyr525/526 in mice. On 16 weeks of feeding, fostamatinib dose-dependently reduces atherosclerotic lesion sizes in aortic roots and arches by up to 59% and 68%, respectively. Fostamatinib normalizes HCD-induced monocytosis and neutrophilia and attenuates T- and B-lymphocyte numbers. Fostamatinib favorably alters plaque composition and inflammation. Fostamatinib treatment causes a significant shift from the proinflammatory Gr-1^high monocyte subtype to the rather antiinflammatory Gr-1^low subtype. Fostamatinib impairs inflammatory cell recruitment to the endothelium. Fostamatinib reduces migration of inflammatory cells. Fostamatinib also impairs macrophage differentiation and survival. ^[3]

Protocols

The R406 prodrug fostamatinib is prepared as a 4 mg/mL solution in 0.1% carboxymethylcellulose sodium, 0.1% methylparaben, and 0.02% propylparaben (pH 6.5). ^[2]

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] Suljagic M, et al. The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the Eµ-TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. Blood. 2010, 116(23): 4894-4905. [3] Hilgendorf I, et al. The oral spleen tyrosine kinase inhibitor fostamatinib attenuates inflammation and atherogenesis in low-density lipoprotein receptor-deficient mice. Arterioscler Thromb Vasc Biol. 2011, 31(9): 1991-1999.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com