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Fostamatinib
| Product Name | Fostamatinib |
| Price: | Inquiry |
| Catalog No.: | CN00172 |
| CAS No.: | 901119-35-5 |
| Molecular Formula: | C23H26FN6O9P |
| Molecular Weight: | 580.46 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | COc1cc(Nc2ncc(c(n2)Nc2ccc3c(n2)N(COP(=O)(O)O)C(=O)C(O3)(C)C)F)cc(c1OC)OC |
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| Description | Fostamatinib (R788), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM. |
| 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]. |
| Density | 1.5±0.1 g/cm3 |
| Boiling Point | 814.2±75.0 °C at 760 mmHg |
| Flash Point | 446.2±37.1 °C |
| Exact Mass | 580.148315 |
| PSA | 199.76000 |
| LogP | 2.12 |
| Vapour Pressure | 0.0±3.1 mmHg at 25°C |
| Storage condition | -20°C |