| Cas No.: | 1025687-58-4 |
| Chemical Name: | sodium (6-((5-fluoro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)-2,2-dimethyl-3-oxo-2H-pyrido[3,2-b][1,4]oxazin-4(3H)-yl)methyl phosphate |
| Synonyms: | R935788; R-935788; R 935788; R788; R 788; R-788 sodium. R935788 sodium. Fostamatinib sodium, Fostamatinib disodium hexahydrate; prodrug of R-406. |
| SMILES: | O1C(C)(C)C(=O)N(COP([O-])([O-])=O)C2=NC(NC3C(F)=CN=C(NC4=CC(OC)=C(OC)C(OC)=C4)N=3)=CC=C12.[Na+].[Na+] |
| Formula: | C23H24FN6Na2O9P |
| M.Wt: | 624.42 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Fostamatinib Disodium (R788 Disodium), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM. |
| 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]. |
| 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]. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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