Fostamatinib disodium
Modify Date: 2024-01-03 09:26:19
Fostamatinib disodium structure
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Common Name | Fostamatinib disodium | ||
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| CAS Number | 1025687-58-4 | Molecular Weight | 624.423 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H24FN6Na2O9P | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Fostamatinib disodiumFostamatinib Disodium (R788 Disodium), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM. |
| Name | 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 |
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| Synonym | More Synonyms |
| Description | Fostamatinib Disodium (R788 Disodium), 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 | 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]. |
| References |
| Molecular Formula | C23H24FN6Na2O9P |
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| Molecular Weight | 624.423 |
| Exact Mass | 624.112183 |
| PSA | 205.42000 |
| LogP | 3.53080 |
| Storage condition | -20℃ |
| Hazard Codes | N |
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| Tamatinib fosdium |
| Disodium [6-({5-fluoro-2-[(3,4,5-trimethoxyphenyl)amino]-4-pyrimidinyl}amino)-2,2-dimethyl-3-oxo-2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl]methyl phosphate |
| Fostamatinib disodium |
| R788 |
| R788(prodrug of R406) |
| 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]-, sodium salt (1:2) |
| Fostamatinib disodium salt |
| S2206_Selleck |
| R788,FosD,tamatinib fosdium |
| R788 Disodium |
| R788 sodium |
| R935788 |
| R788(Disodium) |