CAS 914295-16-2|R788 (disodium hexahydrate)
Introduction：Basic information about CAS 914295-16-2|R788 (disodium hexahydrate), including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | R788 (disodium hexahydrate) | ||
|---|---|---|---|
| CAS Number | 914295-16-2 | Molecular Weight | 732.51 |
| Density | / | Boiling Point | / |
| Molecular Formula | C23H24FN6Na2O9P.6H2O | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | 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-4-[(phosphonooxy)methyl]-, disodium salt, hexahydrate |
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| Synonym | More Synonyms |
R788 (disodium hexahydrate) BiologicalActivity
| Description | Fostamatinib disodium hexahydrate (R788 disodium hexahydrate), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM. |
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| Related Catalog | Signaling Pathways >>Protein Tyrosine Kinase/RTK >>SykResearch Areas >>Inflammation/Immunology |
| Target | IC50 Value: 41 nM [1]Target: Syk |
| In Vitro | 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 | 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]. |
| 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. |
Chemical & Physical Properties
| Molecular Formula | C23H24FN6Na2O9P.6H2O |
|---|---|
| Molecular Weight | 732.51 |
| PSA | 205.76000 |
| LogP | 3.24120 |
| InChIKey | ZQGJCHHKJNSPMS-UHFFFAOYSA-L |
| SMILES | COc1cc(Nc2ncc(F)c(Nc3ccc4c(n3)N(COP(=O)([O-])[O-])C(=O)C(C)(C)O4)n2)cc(OC)c1OC.O.O.O.O.O.O.[Na+].[Na+] |
Synonyms
| FostaMatinib DisodiuM Hexahydrate |
| R788 disodium hexahydrate |
| R788 (disodium hexahydrate) |
