R788 (disodium hexahydrate) structure
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Common Name | R788 (disodium hexahydrate) | ||
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CAS Number | 914295-16-2 | Molecular Weight | 732.51 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C23H24FN6Na2O9P.6H2O | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of R788 (disodium hexahydrate)Fostamatinib disodium hexahydrate (R788 disodium hexahydrate), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM. |
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 |
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 | |
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 |
Molecular Formula | C23H24FN6Na2O9P.6H2O |
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Molecular Weight | 732.51 |
PSA | 205.76000 |
LogP | 3.24120 |
FostaMatinib DisodiuM Hexahydrate |
R788 disodium hexahydrate |
R788 (disodium hexahydrate) |