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R788(prodrug of R406) CAS: 1025687-58-4

Category: Inhibitors
Product Name: R788(prodrug of R406)
Cat No: I000167
CAS No: 1025687-58-4
Synonyms: disodium;[6-[[5-fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl phosphate
Molecular Formula: C23H24FN6O9P • 2Na
Molecular Weight: 624.4
SMILES: COC1=C(OC)C=C(NC2=NC(NC3=NC(N(COP([O-])([O-])=O)C(C(C)(C)O4)=O)=C4C=C3)=C(F)C=N2)C=C1OC.[Na+].[Na+]
Solubility: DMSO <1.2mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
Target: Spleen Tyrosine Kinase (Syk)
IC50: 41 nM
Storage: powder
CAS 1025687-58-4,R788(prodrug of R406)
  • Description

R788 (Fostamatinib) disodium, a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.

in vitro: R788 is a methylene phosphate prodrug of R406, which can be rapidly converted to R406 in vivo. R406 (in vitro active form of R788) selectively inhibits Syk-dependent signaling with EC50 values ranging from 33 nM to 171 nM, more potently than Syk-independent pathways in different cells [1]. R406 inhibits cellular proliferation of a variety of diffuse large B-cell lymphoma (DLBCL) cell lines with EC50 values ranging from 0.8 μM to 8.1 μM [2]. R406 treatment reduces basal phosphorylation of BLNK, Akt, glycogen synthase kinase-3 (GSK-3), forkhead box O (FOXO) and ERK not only in cells with high (TCL-002) but also in cells with low levels of phosphorylated Syk (TCL1-551). In addition, R406 completely inhibits the anti-IgM induced Bcr signal in TCL1 leukemias. Despite the higher levels of constitutively active Syk in TCL1 leukemias, R406 is not selectively cytotoxic to the leukemic cells [3]. 

in vivo: R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals [3]. 

  • Spec

Appearance:A crystalline solid

  • 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): p. 998-1008. 

[2]. Chen, L., et al., SYK-dependent tonic B-cell receptor signaling is a rational treatment target in diffuse large B-cell lymphoma. Blood, 2008. 111(4): p. 2230-7. 

[3]. Suljagic, M., et al., The Syk inhibitor fostamatinib disodium (R788) inhibits tumor growth in the Emu- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. Blood, 2010. 116(23): p. 4894-905.

price inquiry for CAS:1025687-58-4, Product:R788(prodrug of R406)