| Cas No.: | 901119-35-5 |
| Chemical Name: | R 788,R-788，R788 |
| Synonyms: | R 788,R-788，R788 |
| SMILES: | COC1=CC(NC2=NC=C(C(NC3=NC(N4COP(O)(O)=O)=C(C=C3)OC(C)(C)C4=O)=N2)F)=CC(OC)=C1OC |
| Formula: | C23H26FN6O9P |
| M.Wt: | 580.46 |
| Sotrage: | 4°C for 1 year, -20°C for more than 2 years |
| Description: | Fostamatinib (R788), 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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