1025687-58-4
1025687-58-4 structure
- Name: Fostamatinib disodium
- Chemical 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
- CAS Number: 1025687-58-4
- Molecular Formula: C23H24FN6Na2O9P
- Molecular Weight: 624.423
- Catalog: Biochemical Inhibitor Angiogenesis Syk inhibitor
- Create Date: 2016-03-05 21:30:37
- Modify Date: 2025-08-20 19:36:35
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Fostamatinib 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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| Synonyms |
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) |
| 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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